S1166 |
Cisplatin
|
Cisplatin is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation. |
-
Nat Cancer, 2024, 10.1038/s43018-024-00814-0
-
Nat Commun, 2024, 15(1):5775
-
Nat Commun, 2024, 15(1):2853
|
|
S7418 |
Cycloheximide
|
Cycloheximide, an antifungal antibiotic, is an eukaryote protein synthesis inhibitor with IC50 of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively. Cycloheximide suppresses ferroptosis and inhibits autophagy.Solutions are unstable and should be fresh-prepared.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing. |
-
Signal Transduct Target Ther, 2024, 9(1):65
-
Mol Cancer, 2024, 23(1):143
-
Cell Metab, 2024, 36(7):1598-1618.e11
|
|
S1714 |
Gemcitabine
|
Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis. |
-
Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
-
Drug Resist Updat, 2024, 74:101079
-
Nat Commun, 2024, 15(1):1287
|
|
S1209 |
5-FU (5-Fluorouracil)
|
5-FU (5-Fluorouracil) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV. |
-
Mol Cancer, 2024, 23(1):186
-
Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
-
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
|
|
S1224 |
Oxaliplatin
|
Oxaliplatin is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation. |
-
Mol Cancer, 2024, 23(1):186
-
Mol Cancer, 2024, 23(1):23
-
Gastroenterology, 2024, S0016-5085(24)00062-3
|
|
S1237 |
TMZ(Temozolomide)
|
TMZ(Temozolomide) is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells. Temozolomide induces apoptosis and exhibits antitumor activity. |
-
Cell Discov, 2024, 10(1):39
-
Cell Death Dis, 2024, 15(3):205
-
NPJ Precis Oncol, 2024, 8(1):59
|
|
S1491 |
Fludarabine
|
Fludarabine is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis. |
-
Nat Commun, 2024, 15(1):1718
-
Cell Rep Med, 2024, 5(2):101420
-
Cell Death Dis, 2024, 15(8):600
|
|
S1149 |
Gemcitabine HCl
|
Gemcitabine HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively. |
-
Int J Biol Sci, 2024, 20(4):1389-1409
-
Phytomedicine, 2024, 155377
-
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
|
|
S1215 |
Carboplatin
|
Carboplatin, a derivative of CDDP, is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death and interfers with the cell's repair mechanism in A2780, SKOV-3, IGROV-1, and HX62 cells. It induces the formation of DNA interstrand crosslinks and DNA-protein crosslinks. Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation. |
-
Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
-
Nat Commun, 2024, 15(1):1158
-
Cell Rep Med, 2024, S2666-3791(24)00201-5
|
|
S1214 |
Bleomycin sulfate
|
Bleomycin sulfate is a glycopeptide antibiotic and a DNA synthesis inhibitor, as well as an anticancer agent for squamous cell carcinomas (SCC) with an IC50 of 4 nM in UT-SCC-19A cells. Bleomycin sulfate is a DNA synthesis inhibitor. |
-
Bioact Mater, 2024, 32:488-501
-
Nat Commun, 2024, 15(1):1429
-
EMBO J, 2024, 43(1):61-86
|
|
S8146 |
Mitomycin C
|
Mitomycin C (Ametycine) is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers. Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95-independent manner.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing. |
-
Nucleic Acids Res, 2024, gkae740
-
Clin Transl Med, 2024, 14(2):e1586
-
J Neuroinflammation, 2024, 21(1):136
|
|
S1117 |
Triciribine (API-2)
|
Triciribine (API-2) is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2. |
-
J Cell Sci, 2023, 136(4)jcs259788
-
Exp Gerontol, 2023, 173:112091
-
EJHaem, 2023, 4(3):631-638
|
|
S8932 |
Remdesivir (GS-5734)
|
Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV. |
-
Antiviral Res, 2024, 225:105840
-
Int J Mol Sci, 2024, 25(3)1427
-
Int J Mol Sci, 2024, 24;25(3):1427.
|
|
S1648 |
Cytarabine
|
Cytarabine is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis. |
-
Nat Commun, 2024, 15(1):4739
-
Blood Adv, 2024, 8(20):5315-5329
-
iScience, 2024, 27(1):108667
|
|
S3035 |
Daunorubicin HCl
|
Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis. |
-
Nat Commun, 2024, 15(1):4739
-
Haematologica, 2024, 109(6):1713-1725
-
Int J Oncol, 2024, 64(6)66
|
|
S2684 |
Pidnarulex (CX-5461)
|
Pidnarulex (CX-5461) is an inhibitor of rRNA synthesis, selectively inhibits Pol I-driven transcription of rRNA with IC50 of 142 nM in HCT-116, A375, and MIA PaCa-2 cells, has no effect on Pol II, and possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation. |
-
Mol Cell, 2024, 84(8):1527-1540.e7
-
Cell Rep Med, 2024, 5(10):101778
-
Sci Rep, 2024, 14(1):4060
|
|
S1229 |
Fludarabine Phosphate
|
Fludarabine Phosphate is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis. |
-
J Autoimmun, 2024, 149:103307
-
Cell Death Dis, 2024, 15(3):224
-
J Biomed Sci, 2022, 29(1):20
|
|
S1135 |
Pemetrexed disodium
|
Pemetrexed disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis. |
-
Cell Death Dis, 2024, 15(8):555
-
Cell Commun Signal, 2024, 22(1):375
-
Cancer Cell, 2022, 40(10):1128-1144.e8
|
|
S1896 |
Hydroxyurea
|
Hydroxyurea is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection. |
-
Nat Commun, 2024, 15(1):7360
-
iScience, 2024, 27(4):109580
-
Sci Adv, 2024, 10(21):eadk8908
|
|
S2794 |
Sofosbuvir
|
Sofosbuvir is a HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection. |
-
J Med Virol, 2024, 96(7):e29787
-
PLoS One, 2024, 19(5):e0303265
-
mBio, 2023, 10.1128/mbio.01318-23
|
|
S1212 |
Bendamustine HCl
|
Bendamustine HCl is a DNA-damaging agent with IC50 of 50 μM in cell-free assay. |
-
Res Sq, 2024, rs.3.rs-3848777
-
Cell Death Discov, 2023, 9(1):39
-
Front Immunol, 2022, 13:1045710
|
|
S7742 |
SCR7
|
SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ). It increases the efficiency of HDR-mediated genome editing up to 19-fold using CRISPR/Cas9 in mammalian cells and mouse embryos. |
-
iScience, 2024, 27(2):108814
-
Nat Commun, 2023, 14(1):4761
-
Nat Commun, 2023, 14(1):4761
|
|
S2239 |
Tubacin
|
Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1. Tubacin reduces the replication of the Japanese Encephalitis Virus via the decrease of viral RNA synthesis. |
-
Dev Cell, 2024, S1534-5807(24)00326-5
-
Br J Cancer, 2023, 10.1038/s41416-023-02195-0
-
Int J Mol Sci, 2023, 24(5)4720
|
|
S1156 |
Capecitabine
|
Capecitabine is a tumor-selective fluoropyrimidine carbamate, which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU. Capecitabine treatment of HCT-15 cells causes condensation of DNA and induces apoptosis. |
-
Genes Dis, 2024, 11(1):430-448
-
Naunyn Schmiedebergs Arch Pharmacol, 2024, 10.1007/s00210-024-03145-0
-
J Pers Med, 2022, 12(2)258
|
|
S5971 |
Pemetrexed
|
Pemetrexed (LY231514) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis. |
-
Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
-
Cell Rep Med, 2024, 5(7):101615
-
Mol Cancer Res, 2024, 22(1):82-93
|
|
S1373 |
Daptomycin
|
Daptomycin is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms. |
-
Molecules, 2023, 28(2)621
-
Infect Drug Resist, 2023, 16:4867-4879
-
Infect Drug Resist, 2023, 16:4867-4879
|
|
S1199 |
Cladribine
|
Cladribine is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively. |
-
Oncotarget, 2024, 15:220-231
-
Exp Hematol Oncol, 2023, 12(1):23
-
Neurol Neuroimmunol Neuroinflamm, 2023, 10(5)e200149
|
|
S7419 |
Blasticidin S HCl
|
Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes. It acts by blocking hydrolysis of peptidyl-tRNA induced by release factors and inhibits peptide bond formation. It is used to select transfected cells carrying bsr or BSD resistance genes. |
-
Nucleic Acids Res, 2024, gkae787
-
Cell Rep Med, 2024, 5(5):101533
-
Pharmacol Res, 2024, 206:107283
|
|
S5582 |
Cytarabine hydrochloride
|
Cytarabine is a pyrimidine nucleoside analog that is used mainly in the treatment of leukemia. It is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. |
-
Blood, 2022, blood.2022016090
-
Clin Transl Med, 2022, 12(2):e722
-
Front Pharmacol, 2022, 13:1032975
|
|
S7975 |
Favipiravir (T-705)
|
Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.
|
-
J Med Virol, 2024, 96(1):e29372
-
Okayama University, 2023 , 10.18926/65391
-
Nat Commun, 2022, 13(1):2256
|
|
S3190 |
m6A (N6-methyladenosine)
|
m6A (N6-methyladenosine) is a base modified analog of adenosine and is found as a minor nucleoside in natural RNAs. |
-
Biosci Rep, 2024, 44(1)BSR20231430
-
Nucleic Acids Res, 2023, 51(2):517-535
-
Oncol Rep, 2023, 49(5)94
|
|
S1218 |
Clofarabine
|
Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis. |
-
Front Oncol, 2023, 13:1287444
-
Cancer Res, 2022, 82(4):721-733
-
Clin Transl Med, 2022, 12(2):e747
|
|
S8246 |
RK-33
|
RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells. |
-
Cell Rep, 2024, 43(3):113937
-
JCI Insight, 2023, 8(7)e167566
-
Mol Immunol, 2023, 154:54-60
|
|
S1840 |
Lomustine
|
Lomustine (NSC79037, Gleostine, CeeNU, CCNU) inhibits cancer cells by damaging the DNA and stops cells from dividing. |
-
Sci Rep, 2024, 14(1):4303
-
Cell Rep Med, 2023, S2666-3791(23)00156-8
-
Mol Biol Cell, 2023, 34(5):ar47
|
|
S1302 |
Ifosfamide
|
Ifosfamide is a nitrogen mustard alkylating agent used in the treatment of cancer. |
-
Cancer Res, 2023, 83(16):2750-2762
-
Comput Struct Biotechnol J, 2023, 21:3827-3840
-
Comput Struct Biotechnol J, 2023, 21:3827-3840
|
|
S1807 |
Acyclovir (Aciclovir)
|
Acyclovir (Aciclovir) is a synthetic nucleoside analogue active against herpesviruses. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells. |
-
Cell, 2023, 186(14):3033-3048.e20
-
iScience, 2022, 25(12):105682
-
Pharmaceutics, 2022, 14(3)536
|
|
S1289 |
Carmofur
|
Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer. |
-
JCI Insight, 2023, 8(9)e166850
-
Cell Death Discov, 2023, 9(1):451
-
Int J Mol Sci, 2023, 24(7)6062
|
|
S7470 |
Triapine (3-AP)
|
Triapine (3-AP) is a potent ribonucleotide reductase (RNR) inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2. |
-
J Virol, 2023, 97(8):e0026723
-
Res Sq, 2023, rs.3.rs-3126261
-
Cancer Res, 2022, 82(4):721-733
|
|
S1192 |
Raltitrexed
|
Raltitrexed (ZD-1694) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth. |
-
Mol Ther, 2022, S1525-0016(22)00717-1
-
ACS Chem Neurosci, 2022, 13(17):2646-2657
-
Biochem Biophys Res Commun, 2022, 610:1-7
|
|
S1221 |
Dacarbazine
|
Dacarbazine is a triazene derivative with antineoplastic activity. Dacarbazine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis; used in the treatment of various cancers. |
-
Cell Death Dis, 2023, 14(6):348
-
BMC Complement Med Ther, 2023, 23(1):111
-
BMC Complement Med Ther, 2023, 23(1):111
|
|
S1305 |
Mercaptopurine (6-MP)
|
Mercaptopurine(6-MP) is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA. |
-
Nat Commun, 2023, 14(1):5913
-
Nat Commun, 2023, 14(1):5913
-
J Pers Med, 2022, 12(2)258
|
|
S8434 |
B02
|
B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM). |
-
iScience, 2024, 27(2):108814
-
Cell Prolif, 2023, 56(4):e13384
-
Cancer Med, 2023, 12(6):6594-6602
|
|
S7718 |
BMH-21
|
BMH-21 is a DNA intercalator, which binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.
|
-
Nucleic Acids Res, 2024, gkae316
-
Elife, 2024, 13e80684
-
J Biol Chem, 2024, 300(3):107115
|
|
S1213 |
Nelarabine
|
Nelarabine (506U78,Arranon) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells. |
-
Cancer Res, 2022, 82(4):721-733
-
Cell Rep, 2022, 39(10):110913
-
J Pers Med, 2022, 12(2)258
|
|
S7679 |
YK-4-279
|
YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).
|
-
Nat Commun, 2024, 15(1):4590
-
Cancers -Basel), 2023, 15(19)4772
-
Cell Chem Biol, 2022, 29(8):1325-1332.e4
|
|
S1764 |
Rifampin (Rifampicin)
|
Rifampin (Rifampicin) is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections. |
-
Cell Death Dis, 2023, 14(1):64
-
Int J Mol Sci, 2022, 23(13)7383
-
Biomedicines, 2021, 9(8)996
|
|
S1299 |
Floxuridine (FUDR)
|
Floxuridine (FUDR) is a prodrug that is rapidly catabolized to 5-fluorouracil in vivo. Floxuridine is used to treat various cancers, particularly metastases to the liver. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage and apoptosis. Floxuridine has antiviral effects against HSV and CMV. |
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Cell Chem Biol, 2021, S2451-9456(21)00306-8
|
|
S7918 |
BrdU (Bromodeoxyuridine)
|
BrdU (Bromodeoxyuridine) is a nucleoside analog that competes with thymidine for incorporation into DNA, and used in the detection of proliferating cells.
|
-
CNS Neurosci Ther, 2024, 30(6):e14800
-
Heliyon, 2024, 10(3):e24779
-
Int J Ophthalmol, 2024, 17(6):1018-1027
|
|
S1949 |
Menadione (Vitamin K3)
|
Menadione (Vitamin K3), a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement. |
-
Med -N Y, 2022, S2666-6340-2200365-8
-
Mol Cell, 2021, S1097-2765(21)00269-0
-
DNA Repair (Amst), 2021, 105:103152
|
|
S1995 |
Procarbazine HCl
|
Procarbazine HCl (NSC-77213) is a hydrochloride salt form of procarbazine which is a polyfunctional alkylating compound, used for the treatment of Hodgkin's lymphoma. |
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 34(6):1911-1918
|
|
S4239 |
Bergapten
|
Bergapten is a psoralen that can be photoactivated and is capable of crossing-linking DNA, covalently modifying proteins and lipids, and consequently inhibiting cell replication. |
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 10.1007/s13577-021-00579-z
|
|
S4288 |
Chloroambucil
|
Chloroambucil (Chlorambucil,CB-1348,WR-139013) is a nitrogen mustard alkylating agent, used in the treatment of chronic lymphocytic leukemia.
|
-
bioRxiv, 2023, 2023.01.17.524444
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S1516 |
Cidofovir
|
Cidofovir suppresses virus replication by selective inhibition of viral DNA synthesis. |
-
Oncol Lett, 2021, 21(4):280
-
Nat Biotechnol, 2019, 37(3):303-313
-
Antiviral Res, 2019, 162:178-185
|
|
S2678 |
NSC 207895
|
NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase. |
-
PLoS One, 2024, 19(1):e0295629
-
Front Oncol, 2021, 11:582511
-
Genes Dev, 2020, 34(7-8):526-543
|
|
S1778 |
Trifluridine (NSC 75520)
|
Trifluridine (NSC 529182, NSC 75520, Viroptic, Trifluorothymidine, TFT) is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye. |
-
Nat Med, 2023, 29(3):605-614
-
JCI Insight, 2022, 7(22e158060)
-
Biochem Biophys Res Commun, 2022, 610:119-126
|
|
S1300 |
Tegafur (FT-207)
|
Tegafur (NSC 148958,Fluorafur,FT-207) is a substance being used in the treatment of some types of cancer. |
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 34(6):1911-1918
|
|
S4194 |
Azaguanine-8
|
Azaguanine-8 (NSC-749, SF-337, SK 1150) is a purine analogs showing antineoplastic activity by competing with guanine in the metabolism. |
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 10.1007/s13577-021-00579-z
|
|
S8144 |
Halofuginone
|
Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal. |
-
Cell Rep, 2024, 43(9):114728
-
J Neurochem, 2024, 10.1111/jnc.16102
-
Infect Agent Cancer, 2023, 18(1):27
|
|
S1983 |
Adenine HCl
|
Adenine HCl(6-Aminopurine hydrochloride) is a hydrochloride salt form of adenine which is a purine derivative and a nucleobase with a variety of roles in biochemistry. |
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 34(6):1911-1918
|
|
S4227 |
Fidaxomicin
|
Fidaxomicin is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit. |
-
J Antimicrob Chemother, 2024, dkae101
-
Nucleic Acids Res, 2023, 51(19):e99
-
bioRxiv, 2023, 2023.03.13.532464
|
|
S1384 |
Mizoribine
|
Mizoribine is an imidazole nucleoside and an immunosuppressant that inhibits HCV RNA replication with IC50 of ~ 100 μM for anti-HCV activity. Mizoribine is a selective inhibitor of inosine-5'-monophosphate dehydrogenase (IMPDH) and guanosine monophosphate synthetase. Mizoribine also inhibits SARS-CoV. |
-
EMBO J, 2023, e110620.
-
bioRxiv, 2022, 2021.07.02.450964
-
Cell Death Differ, 2021, 10.1038/s41418-021-00853-5
|
|
S4297 |
Mupirocin
|
Mupirocin(BRL-4910A,Pseudomonic acid) is an isoleucyl t-RNA synthetase inhibitor, used in the treatment of bacterial skin infections.
|
-
Infect Drug Resist, 2023, 16:4867-4879
-
Infect Drug Resist, 2023, 16:4867-4879
-
Anaerobe, 2020, 62:102169
|
|
S1217 |
Cyclophosphamide
|
Cyclophosphamide(NSC 26271,Endoxan, Cytoxan, Neosar, Procytox, Revimmune, Cytophosphane) is a nitrogen mustard alkylating agent from the oxazophorines group. |
-
J Immunother, 2024, 10.1097/CJI.0000000000000505
-
Oncol Lett, 2024, 27(4):158
-
Stem Cell Res Ther, 2023, 14(1):75
|
|
S1973 |
Cyclocytidine HCl
|
Cyclocytidine (NSC 145668) is the prodrug of cytarabine, which is a pyrimidine nucleoside analog that inhibits the DNA synthesis and used mainly in the treatment of leukemia. |
-
Transl Oncol, 2023, 35:101712
-
PeerJ, 2022, 10:e13719
-
Acta Biochim Biophys Sin (Shanghai), 2020, 14 pii: gmaa017
|
|
S4803 |
Thymidine
|
Thymidine is a pyrimidine nucleoside that is composed of the pyrimidine base thymine attached to the sugar deoxyribose. As a constituent of DNA, thymidine pairs with adenine in the DNA double helix. |
-
Nat Commun, 2024, 15(1):2371
-
EBioMedicine, 2024, 103:105129
-
Sci Adv, 2024, 10(21):eadk8908
|
|
S2029 |
Uridine
|
Uridine (NSC 20256,β-Uridine, Uridin) is a nucleoside, contains a uracil attached to a ribose ring via a β-N1-glycosidic bond. |
-
Cancer Res, 2022, canres.1707.2021
-
iScience, 2022, 25(5):104293
-
J Med Chem, 2021, 64(18):13918-13932
|
|
S5948 |
Amodiaquine
|
Amodiaquine is a synthetic aminoquinoline that acts by binding to the protozoal or parasitic DNA and preventing DNA and RNA production and subsequent protein synthesis. It is used for the therapy of malaria. |
-
Molecules, 2024, 29(6)1363
-
Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
-
bioRxiv, 2020, 10.1101/2020.04.13.039917
|
|
S1907 |
Metronidazole
|
Metronidazole, a synthetic antibacterial and antiprotozoal agent of the nitroimidazole class, is used against protozoa. |
-
Microorganisms, 2022, 10(7)1421
-
Elife, 2021, 10e69795
-
Bone Joint Res, 2020, 16;9(4):152-161
|
|
S1760 |
Rifapentine
|
Rifapentine (MDL473) is an antibiotic, which inhibits DNA-dependent RNA polymerase activity, used to treat tuberculosis. |
-
Int J Mol Sci, 2022, 23(13)7383
-
Front Microbiol, 2020, 10:2936
-
mSphere, 2018, 3(5)
|
|
S1784 |
Vidarabine
|
Vidarabine is an antiviral drug by interfering with the synthesis of viral DNA, used to treat herpes simplex and varicella zoster viruses. |
-
Neuron, 2017, 96(6):1290-1302
-
ACS Appl Mater Interfaces, 2016, 8(39):25818-25824
-
Biogerontology, 2016, 17(5-6):907-920
|
|
S1826 |
Nedaplatin
|
Nedaplatin(NSC 375101D) is a derivative of cisplatin and DNA damage agent for tumor colony forming units with IC50 of 94 μM.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation. |
-
Nat Commun, 2019, 10(1):5654
-
Cancer Res, 2018, 78(19):5694-5705
-
Oncol Lett, 2016, 12(5):4195-4202
|
|
S7445 |
APX-3330
|
APX-3330 (E3330) is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.
|
-
J Transl Med, 2023, 21(1):183
-
Cell Death Dis, 2022, 13(2):124
-
Cancer Research on Prevention and Treatment, 2020, (7): 492-497
|
|
S1334 |
Flupirtine maleate
|
Flupirtine maleate is the salt form of Flupirtine, which is a centrally acting non-opioid analgesia, is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. |
-
Assay Drug Dev Technol, 2019, 17(7):310-321
-
Elife, 2015, 4
|
|
S7757 |
6-Thio-dG
|
6-thio-dG (β-TGdR) is a nucleoside analog and telomerase substrate.
|
-
Cell Death Discov, 2024, 10(1):381
-
Radiation Medicine and Protection, 2022, 64-71
-
Clin Sci (Lond), 2020, 10.1042/CS20190890
|
|
S9521 |
Pentostatin
|
Pentostatin(CI-825,Deoxycoformycin) is a potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, particularly hairy-cell leukemia. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity. |
-
Res Sq, 2023, rs.3.rs-2276903
-
Nat Metab, 2020, 10.1038/s42255-020-0227-4
|
|
S8539 |
TAS-102
|
TAS-102 (Trifluridine-Tipiracil Hydrochloride Mixture) is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride. |
-
STAR Protoc, 2024, 5(2):103090
-
J Exp Clin Cancer Res, 2023, 42(1):8
-
Adv Sci (Weinh), 2021, e2103360
|
|
S3669 |
Carmustine
|
Carmustine (bis-chloroethylnitrosourea, BCNU, BiCNU) is a cell-cycle phase nonspecific alkylating antineoplastic agent and used in the treatment of brain tumors and various other malignant neoplasms. |
-
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
-
Cancer Res, 2021, 81(23):6044-6057
|
|
S8850 |
JH-RE-06
|
JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS). |
-
Nucleic Acids Res, 2024, gkae317
-
Nucleic Acids Res, 2024, gkae785
-
Cell Rep, 2024, 43(5):114205
|
|
S7546 |
Pritelivir (BAY 57-1293)
|
Pritelivir (BAY 57-1293, AIC316) is a potent helicase primase inhibitor, exhibiting antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2.
|
-
PLoS Pathog, 2021, 17(11):e1010117
-
J Virol, 2021, JVI0166621
|
|
S9718 |
TK216
|
TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. TK216 exhibits antilymphoma activity.
|
-
J Biol Chem, 2024, 300(6):107375
-
Sci Rep, 2023, 13(1):14360
-
Sci Rep, 2023, 13(1):14360
|
|
S1790 |
Rifaximin
|
Rifaximin is a RNA synthesis inhibitor by binding the β subunit of the bacterial DNA-dependent RNA polymerase, used to treat traveler's diarrhea caused by certain bacteria. |
-
Int J Mol Sci, 2022, 23(13)7383
|
|
S5552 |
Amenamevir
|
Amenamevir (ASP2151) is a potent helicase-primase inhibitor and a novel class of antiviral agent. |
-
J Biomol Struct Dyn, 2020, 1-14
|
|
S0280 |
Madrasin
|
Madrasin (DDD00107587) is a potent and cell-penetrant pre-mRNA splicing inhibitor. Madrasin interferes with the early stages of spliceosome assembly and stalls spliceosome assembly at the A complex. |
-
Leukemia, 2023, 37(8):1649-1659
|
|
S8095 |
Tubercidin
|
Tubercidin (7-deaza-adenosine), an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities. |
-
Mol Cell, 2020, 80(6):1104-1122.e9
|
|
S5484 |
Rimantadine Hydrochloride
|
Rimantadine is an RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. It works by inhibiting a viral protein called M2, which normally mediates the transport of acid ions across the influenza virion shell. |
-
bioRxiv, 2020, 2020.08.12.246389
|
|
S3168 |
cis-Resveratrol
|
cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
-
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
|
|
S4737 |
Psoralen
|
Psoralen (Psoralene, Ficusin, Furocoumarin) is a naturally occurring furocoumarin that intercalates with DNA, inhibiting DNA synthesis and cell division. |
-
Metabolites, 2022, 13(1)3
|
|
E0488 |
BC-LI-0186
|
BC-LI-0186 is a selective blocker of Leucyl-tRNA synthetase (LRS, LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (LRS-RagD interaction) (IC50 = 46.11 nM) by competing against RagD for LRS VC domain binding (KD = 42.1 nM), thereby inhibiting lysosomal localization of LRS and mTORC1 activity. It also effectively suppresses the activity of cancer-associated mTOR mutants and the growth of rapamycin-resistant cancer cells. |
-
Cancer Res Treat, 2023, 55(3):851-864
|
|
S5953 |
Menadione bisulfite sodium
|
Menadione(Vitamin K3) bisulfite sodium, a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement. |
-
Life Sci, 2020, 242:117159
|
|
S7449 |
CRT0044876
|
CRT0044876 (NSC 69877, 7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM. |
-
Cell Rep, 2024, 43(10):114820
-
Nat Biotechnol, 2017, 35(5):463-474
|
|
S3549 |
PFM01
|
PFM01, a cell-permeable N-alkylated Mirin derivative, is a selective inhibitor of MRE11 endonuclease activity. |
-
Cell Rep, 2023, 42(7):112792
|
|
S7637 |
DTP3
|
DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway. |
-
Life Sci Alliance, 2024, 7(8)e202302555
-
MedComm (2020), 2023, 4(3):e269
|
|
S1981 |
Adenine
|
Adenine(6-Aminopurine) is a purine derivative and a nucleobase with a variety of roles in biochemistry. |
-
PLoS Pathog, 2020, 16;16(3):e1008341
|
|
S6854 |
Triazavirin (TZV)
|
Triazavirin (TZV) is a novel antiviral drug, a nucleoside analogue of nucleic acid that inhibits the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is active against influenza and a number of other viruses. Triazavirin is an effective protective agent on the transmission stage of influenza. |
-
Nature, 2022, 604(7904):120-126
|
|
S0469 |
ML216
|
ML216 (CID-49852229) is a potent and selective inhibitor of the DNA unwinding activity of BLM(Bloom’s syndrome protein) with antitumor activity. ML216 inhibits helicases with IC50 of 0.97 μM and 2.98 μM for BLM636-1298 and BLMfull-length, respectively. |
-
Elife, 2024, 13RP99026
-
Cells, 2022, 12(1)145
|
|
S3001 |
Clevudine
|
Clevudine(Levovir,L-FMAU) is an antiviral drug for the treatment of hepatitis B. |
-
J Biomed Sci, 2024, 31(1):34
|
|
E2939 |
Didox
|
Didox (3,4-dihydroxy-benzohydroxamic acid) is a synthetic ribonucleotide reductase (RR) inhibitor derived from polyhydroxy-substituted benzohydroxamic acid. Didox inhibits proliferation of resistant breast cancer cells. |
|
|
S3009 |
Menthone
|
Menthone is one of the main volatile components of the essential oil of peppermint (Mentha piperita L.). Menthone is used as antioxidant agent and has a good compensatory effect with significant reduction in DNA damages in sperm cells.
|
|
|
S3472 |
Metarrestin
|
Metarrestin is an orally active and specific perinucleolar compartment (PNC) inhibitor that disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription. Metarrestin blocks metastatic development and extends survival in mouse cancer models. |
|
|
E1152 |
AGX51
|
AGX51, a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader, inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability, also inhibits pathologic ocular neovascularization. |
|
|
S8376 |
Rbin-1
|
Rbin-1 (Ribozinoindole-1) is a potent chemical inhibitor of eukaryotic ribosome assembly. It inhibits recombinant full-length Mdn1's ATPase activity in vitro. |
|
|
S6909 |
Levomefolic acid
|
Levomefolic acid (5-MTHF, LMSR, Metafolin, Nutrifolin) is a natural, active form of folic acid used at the cellular level for DNA reproduction, the cysteine cycle and the regulation of homocysteine among other functions. |
|
|
E0459 |
Robinetin
|
Robinetin inhibits HIV integrase cleavage and integration in a dose-dependent manne, inhibits the DNA synthesis in Proteus vulgaris, and the RNA synthesis in S. aureus, also inhibits egg yolk phosphatidylcholine (EYPC) membrane lipid peroxidation and hemoglobin A (HbA) glycosylation with high efficiency. |
|
|
E1596 |
AOH1996
|
AOH1996 is an orally active small-molecule PCNA inhibitor with potential anti-tumor activity. It enhances the interaction between PCNA and RPB1, the largest subunit of RNA polymerase II. |
|
|
S0816 |
Brr2 Inhibitor C9
|
Brr2 inhibitor C9 (Brr2 Inhibitor 9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa a group of progressive retinal degenerative disorders. |
|
|
E1528New |
RP-6685
|
RP-6685 is a potent, selective, and orally active inhibitor of DNA polymerase theta (Polθ). RP-6685 exhibits antitumor efficacy in animal models. |
|
|
S4888 |
Guanine
|
Guanine is one of the four main nucleobases found in the nucleic acids DNA and RNA. |
|
|
S9775 |
SCR130
|
SCR130 is a novel DNA repair inhibitor with IC50s of 14 μM in Reh cells and 2 μM in Nalm6 cells. SCR130 specifically inhibits DNA Ligase IV‐mediated joining with minimal or no effect on Ligase III and Ligase I mediated joining. |
|
|
S5813 |
Isoginkgetin
|
Isoginkgetin is a naturally derived biflavonoid with anti-tumor activity. Isoginkgetin directly inhibits the chymotrypsin-like, trypsin-like, and caspase-like activities of the 20S proteasome. Isoginkgetin also is a general inhibitor of Pre-mRNA splicing. |
-
Cell Death Dis, 2024, 15(4):289
-
Cell Death Dis, 2024, 15(4):289
|
|
S8328 |
CeMMEC1 HCl
|
CeMMEC1 is an N-methylisoquinolinone derivative that inhibits the second bromodomain of TAF1 (IC50=0.9 μM). |
|
|
S0054 |
D-I03
|
D-I03 is a selective inhibitor of RAD52 with Kd of 25.8 µM. D-I03 inhibits ssDNA annealing by RAD52 and D-loop formation with IC50 of 5 µM and 8 µM, respectively. |
|
|
S0063 |
RG3039
|
RG3039 (PF-06687859, PF 6687859, Quinazoline 495) is an orally bioavailable and brain-penetrant inhibitor of the mRNA decapping enzyme DcpS with IC50 of 4.2 nM and IC90 of 40 nM, respectively. |
|
|
S4504 |
6-Mercaptopurine (6-MP) Monohydrate
|
6-Mercaptopurine (6-MP) Monohydrate is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.
|
|
|
S5505 |
2’-deoxyuridine
|
2'-deoxyuridine (dU, 2'-dU) is frequently halogenated to create thymidine analogues useful for studies of DNA synthesis and degradation mechanisms. |
|
|
S9716New |
H3B-8800
|
H3B-8800 is a potent and orally active modulator of SF3B splicing. H3B-8800 interacts directly with the SF3b complex, demonstrating anti-cancer properties. H3B-8800 holds promise for studying acute myeloid leukemia (AML) with SF3B1 mutations. |
|
|
S0780 |
Oncrasin-1
|
Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells. |
|
|
S6359 |
Purine
|
Purine is a heterocyclic aromatic organic compound which plays crucial roles in DNA and RNA. It is also significant components in a number of other important biomolecules, such as ATP, GTP, cyclic AMP, NADH, and coenzyme A. |
|
|
S8942 |
Suramin sodium salt
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatase (PTPases) inhibitor, also is the potent inhibitor of sirtuins, purified topoisomerase II and SARS-CoV-2 RNA-dependent RNA polymerase (RdRp). |
-
J Biol Chem, 2024, S0021-9258(24)00128-5
|
|
S9286 |
Neobavaisoflavone
|
Neobavaisoflavone, isolated from seeds of Psoralea corylifolia, exhibits inhibitory activity against DNA polymerase and platelet aggregation. |
|
|
S6848 |
3'-Fluoro-3'-deoxythymidine (Alovudine)
|
3'-Fluoro-3'-deoxythymidine (Alovudine, CL 184824, FddThd, FLT, MIV-310) is a potent inhibitor of polymerase γ and reverse transcriptase that can be used in the treatment of HIV infection. 3'-Fluoro-3'-deoxythymidine (Alovudine) is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer. |
|
|
E0443 |
LDC195943 (IMT1)
|
LDC195943 (IMT1) is a specific and noncompetitive inhibitor of human mitochondrial RNA polymerase (POLRMT). IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases. |
|
|
E0444 |
LDC203974 (IMT1B)
|
LDC203974 (IMT1B) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. LDC203974 has anti-tumour effects. |
|
|
E1255 |
5-Ethynyluridine
|
5-Ethynyluridine (5-EU) is a cell-permeable nucleoside and can be used to label newly synthesized RNA. |
|
|
S8964 |
Actinomycin D (Dactinomycin)
|
Actinomycin D (Dactinomycin, Act D, RASP-101) is a significant polypeptide antibiotic isolated from soil bacteria of the genus Streptomyces. Actinomycin D (Dactinomycin) inhibits DNA repair and rests the cell cycle at G1 phase with IC50 of 0.42 μM and 0.4 nM, respectively. Actinomycin D is an autophagy activator, induces p53-independent cell death and prolongs survival in high-risk chronic lymphocytic leukemia.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing. |
-
Mol Cancer, 2024, 23(1):186
-
Nat Commun, 2024, 15(1):5209
-
Exp Mol Med, 2024, 10.1038/s12276-024-01315-x
|
|
S9649 |
Acelarin (NUC-1031)
|
Acelarin (NUC-1031, CPF-31, MTL-007, GTPL7389) is a DNA synthesis inhibitor with EC50 of 0.2 nM. |
|
|
E1331 |
SU056
|
SU056 is an inhibitor of Y box binding protein 1 (YB-1) with IC50 of 1.73 μM in Sk0V3 cells. |
-
Cancer Lett, 2024, 602:217197
-
Transl Oncol, 2024, 45:101965
|
|
E1987New |
APX2009
|
APX2009 is a second-generation redox-specific inhibitor of APE1/Ref-1, an essential enzyme in the base excision repair (BER) pathway. APX2009 effectively reduces breast cancer cell proliferation and colony formation. |
|
|
S0102 |
L 189
|
L 189 is a novel human DNA ligase inhibitor with IC50 of 5 μM, 9 μM and 5 μM for hLigI, hLigIII and hLigIV, respectively. L 189 inhibits base excision repair (BER) and non-homologous end joining (NHEJ). L 189 specifically sensitizes cancer cells to DNA damage. |
|
|
S9936 |
ART558
|
ART558 is a potent, selective, low molecular weight, allosteric inhibitor of DNA Polθ with an IC50 of 7.9 nM. |
|
|
S3641 |
Osalmid
|
Osalmid suppresses ribonucleotide reductase (RNR) activity in a concentration-dependent manner, with a 50% RR activity-inhibitory concentration (IC50) of 8.23 μM. |
|
|
S3360 |
Bis(2-ethylhexyl) phthalate
|
Bis(2-ethylhexyl) phthalate (Dioctyl phthalate, DOP, Diplast O, ESBO-D 82, Ergoplast FDO, Ergoplast FDO-S, Etalon) induces DNA strand breaks and gene expression alterations in larval zebrafish Danio rerio. |
|
|
S5293 |
Nimustine Hydrochloride
|
Nimustine Hydrochloride (Nidran) is the hydrochloride salt of nimustine, a nitrosourea with antineoplastic activity that alkylates and crosslinks DNA, thereby causing DNA fragmentation, inhibition of protein synthesis, and cell death. |
|
|
S5297 |
Vidarabine monohydrate
|
Vidarabine (Spongoadenosine, Vira-A) is a nucleoside antibiotic with antiviral acitivity that interferes with the synthesis of viral DNA. It is used to treat herpes simplex and varicella zoster viruses. |
|
|
S6997 |
CHAPS
|
CHAPS is a zwitterionic surfactant that decreases the sequence specificity of the nucleosome. |
|
|
S1126New |
CX-3543(Quarfloxin)
|
Quarfloxin (CX-3543), a fluoroquinolone derivative inhibits RNA pol I activity. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template. |
|
|
E1111 |
VV116
|
VV116, a promising orally administered anti-SARS-CoV-2 nucleoside drug candidate, exerts functions by targeting the viral RNA-dependent RNA polymerase through its nucleoside triphosphate form with an IC50 of 0.67±0.24 μM. |
|
|
S6115 |
Pyridoxal 5′-phosphate hydrate
|
Pyridoxal 5′-phosphate (pyridoxal phosphate, Vitamin B6 phosphate, PAL-P, PLP), a vitamin B6 phosphate, is a coenzyme in a variety of enzymatic reactions. Pyridoxal 5′-phosphate at concentrations < 0.5 mM inhibits of polymerization deoxynucleoside triphosphate catalysed by variety of DNA polymerases isolated from type C RNA tumor viruses. The combination of Pyridoxal 5′-phosphate and NEIL2 will make NEIL2 completely lose its ability to bind damaged DNA. |
|
|
E2921 |
Diethyl Pyrocarbonate
|
Diethyl pyrocarbonate is a potent, non-specific inhibitor of RNase. It has been useful as an in vitro agent, relatively specific for binding to imidazole of histidine. It inhibits central chemosensitivity in rabbit and can modify Ser, Thr, His and Tyr residues. |
|
|
S3356 |
Phosphonoacetic acid
|
Phosphonoacetic acid (PAA) is an active endogenous metabolite that possesses a restricted potential to block DNA biosynthesis. Phosphonoacetic acid exhibits anti-viral activities. |
|
|
S8326 |
Saccharin 1-methylimidazole (SMI)
|
Saccharin 1-methylimidazole (SMI) is considered a general-purpose activator for DNA and RNA synthesis. |
|
|
S0161 |
ML367
|
ML367 is a potent, micromolar inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization. ML367 blocks DNA repair pathways and general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation. |
|
|
S8977 |
BCH001
|
BCH001 is a specific PAPD5 inhibitor that restores telomerase activity and telomere length in dyskeratosis congenita (DC) patient induced pluripotent stem cells. PAPD5 is a noncanonical poly(A) polymerase with an unusual RNA-binding motif. |
|
|
S5828 |
L-Abrine
|
L-Abrine (N-Methyl-L-tryptophan), an extremely toxic toxalbumin found in the seeds of the rosary pea, is a ribosome inhibiting protein. |
|
|
S1982 |
Adenine sulfate
|
Adenine sulfate(Adenine hemisulfate) is a sulfate salt form of adenine which is a purine derivative and a nucleobase with a variety of roles in biochemistry. |
|
|
E0510 |
Cidofovir hydrate
|
Cidofovir hydrate is a selective inhibitor of viral DNA synthesis through the selective inhibition of viral DNA polymerase. |
|
|
E1529 |
ART812
|
ART812 is an orally active DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. |
|
|
S6077 |
Cytidine 5′-triphosphate (disodium salt)
|
Cytidine 5'-triphosphate is a pyrimidine nucleoside triphosphate that is involved in a variety of biochemical reactions. It is used in the synthesis of RNA by RNA polymerases. |
|
|
S9603 |
Lurbinectedin
|
Lurbinectedin, a DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity. Lurbinectedin inhibits RMG1 and RMG2 cell growth with IC50 of 1.25 nM and 1.16 nM, respectively. |
|
|
S6893 |
PIN1 inhibitor API-1
|
PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor with IC50 of 72.3 nM. PIN1 inhibitor API-1 targets Pin1 peptidyl-prolyl isomerase domain and inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 up-regulates miRNA biogenesis by retaining active XPO5 conformation and suppresses HCC development. |
|
|
S4476 |
PCNA-I1
|
PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells. |
|
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S4236 |
Proflavine Hemisulfate
|
Proflavine Hemisulfate is a topical antiseptic by interchelating DNA, thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands. |
|
|
S5374 |
5'-Cytidylic acid
|
5'-Cytidylic acid (Cytidine monophosphate, Cytidine 5'-phosphate) is a nucleotide that is used as a monomer in RNA. |
|
|
S5384 |
UTP Trisodium Salt
|
Uridine-5'-triphosphate (UTP) is a pyrimidine nucleoside triphosphate and a substrate for the synthesis of RNA during transcription. |
|
|
S2600 |
Fexinidazole
|
Fexinidazole (HOE-239, Fexinidazole Winthrop) is a 5-nitroimidazole derivative. Fexinidazole is a DNA synthesis inhibitor and the only, all-oral agent for Human African Trypanosomiasis(HAT or sleeping sickness). |
-
Int J Mol Sci, 2024, 25(8)4413
|
|
S2961 |
GC7 Sulfate
|
GC7 (N1-guanyl-1,7-diaminoheptane) Sulfate is an inhibitor of deoxyhypusine synthase (DHPS). GC7 inhibits Neuroblastoma (NB) cell proliferation in a dose-dependent manner, through induction of the cell cycle inhibitor p21 and reduction of total and phosphorylated Rb proteins. |
-
Exp Mol Med, 2024, 10.1038/s12276-024-01214-1
|
|
S4782 |
5-methoxyflavone
|
5-methoxyflavone is a novel DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. |
|
|
S4537 |
Oxolinic acid
|
Oxolinic acid (Urinox, NSC 110364) is a quinolone antibiotic, inhibiting the enzyme DNA gyrase and DNA synthesis.It also acts as a dopamine reuptake inhibitor. |
|
|
S4423 |
Emamectin Benzoate
|
Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis. |
|
|
E1070 |
Phen-DC3 Trifluoromethanesulfonate
|
Phen-DC3 Trifluoromethanesulfonate is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65 ± 6 and 50 ± 10 nM, respectively. |
|
|
S8329 |
CeMMEC13
|
CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 µM). |
|
|
E0511 |
Framycetin sulphate
|
Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM, and competes for specific divalent metal ion binding sites in RNase P RNA, also inhibits hammerhead ribozyme with a Ki of 13.5 μM. |
|
|
S2427 |
Triglycidyl Isocyanurate (Teroxirone)
|
Triglycidyl Isocyanurate (Teroxirone, Tris(2,3-epoxypropyl) Isocyanurate, TGI, TGIC) is a triazene triepoxide with antineoplastic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl Isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. Triglycidyl Isocyanurate is also used in various polyester powder coatings in the metal finishing industry. |
|
|
S9382 |
Thymine
|
Thymine (5-methyluracil) is one of the four nucleobases in the nucleic acid of DNA. |
|
|
S1166 |
Cisplatin
|
Cisplatin is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation. |
- Nat Cancer, 2024, 10.1038/s43018-024-00814-0
- Nat Commun, 2024, 15(1):5775
- Nat Commun, 2024, 15(1):2853
|
|
S7418 |
Cycloheximide
|
Cycloheximide, an antifungal antibiotic, is an eukaryote protein synthesis inhibitor with IC50 of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively. Cycloheximide suppresses ferroptosis and inhibits autophagy.Solutions are unstable and should be fresh-prepared.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing. |
- Signal Transduct Target Ther, 2024, 9(1):65
- Mol Cancer, 2024, 23(1):143
- Cell Metab, 2024, 36(7):1598-1618.e11
|
|
S1714 |
Gemcitabine
|
Gemcitabine, a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis. |
- Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
- Drug Resist Updat, 2024, 74:101079
- Nat Commun, 2024, 15(1):1287
|
|
S1209 |
5-FU (5-Fluorouracil)
|
5-FU (5-Fluorouracil) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV. |
- Mol Cancer, 2024, 23(1):186
- Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
- Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
|
|
S1224 |
Oxaliplatin
|
Oxaliplatin is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation. |
- Mol Cancer, 2024, 23(1):186
- Mol Cancer, 2024, 23(1):23
- Gastroenterology, 2024, S0016-5085(24)00062-3
|
|
S1491 |
Fludarabine
|
Fludarabine is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis. |
- Nat Commun, 2024, 15(1):1718
- Cell Rep Med, 2024, 5(2):101420
- Cell Death Dis, 2024, 15(8):600
|
|
S1149 |
Gemcitabine HCl
|
Gemcitabine HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively. |
- Int J Biol Sci, 2024, 20(4):1389-1409
- Phytomedicine, 2024, 155377
- Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
|
|
S1215 |
Carboplatin
|
Carboplatin, a derivative of CDDP, is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death and interfers with the cell's repair mechanism in A2780, SKOV-3, IGROV-1, and HX62 cells. It induces the formation of DNA interstrand crosslinks and DNA-protein crosslinks. Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation. |
- Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
- Nat Commun, 2024, 15(1):1158
- Cell Rep Med, 2024, S2666-3791(24)00201-5
|
|
S8146 |
Mitomycin C
|
Mitomycin C (Ametycine) is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers. Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95-independent manner.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing. |
- Nucleic Acids Res, 2024, gkae740
- Clin Transl Med, 2024, 14(2):e1586
- J Neuroinflammation, 2024, 21(1):136
|
|
S1117 |
Triciribine (API-2)
|
Triciribine (API-2) is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2. |
- J Cell Sci, 2023, 136(4)jcs259788
- Exp Gerontol, 2023, 173:112091
- EJHaem, 2023, 4(3):631-638
|
|
S8932 |
Remdesivir (GS-5734)
|
Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV. |
- Antiviral Res, 2024, 225:105840
- Int J Mol Sci, 2024, 25(3)1427
- Int J Mol Sci, 2024, 24;25(3):1427.
|
|
S1648 |
Cytarabine
|
Cytarabine is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis. |
- Nat Commun, 2024, 15(1):4739
- Blood Adv, 2024, 8(20):5315-5329
- iScience, 2024, 27(1):108667
|
|
S3035 |
Daunorubicin HCl
|
Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis. |
- Nat Commun, 2024, 15(1):4739
- Haematologica, 2024, 109(6):1713-1725
- Int J Oncol, 2024, 64(6)66
|
|
S2684 |
Pidnarulex (CX-5461)
|
Pidnarulex (CX-5461) is an inhibitor of rRNA synthesis, selectively inhibits Pol I-driven transcription of rRNA with IC50 of 142 nM in HCT-116, A375, and MIA PaCa-2 cells, has no effect on Pol II, and possesses 250- to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation. |
- Mol Cell, 2024, 84(8):1527-1540.e7
- Cell Rep Med, 2024, 5(10):101778
- Sci Rep, 2024, 14(1):4060
|
|
S1229 |
Fludarabine Phosphate
|
Fludarabine Phosphate is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis. |
- J Autoimmun, 2024, 149:103307
- Cell Death Dis, 2024, 15(3):224
- J Biomed Sci, 2022, 29(1):20
|
|
S1135 |
Pemetrexed disodium
|
Pemetrexed disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis. |
- Cell Death Dis, 2024, 15(8):555
- Cell Commun Signal, 2024, 22(1):375
- Cancer Cell, 2022, 40(10):1128-1144.e8
|
|
S1896 |
Hydroxyurea
|
Hydroxyurea is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection. |
- Nat Commun, 2024, 15(1):7360
- iScience, 2024, 27(4):109580
- Sci Adv, 2024, 10(21):eadk8908
|
|
S2794 |
Sofosbuvir
|
Sofosbuvir is a HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection. |
- J Med Virol, 2024, 96(7):e29787
- PLoS One, 2024, 19(5):e0303265
- mBio, 2023, 10.1128/mbio.01318-23
|
|
S7742 |
SCR7
|
SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ). It increases the efficiency of HDR-mediated genome editing up to 19-fold using CRISPR/Cas9 in mammalian cells and mouse embryos. |
- iScience, 2024, 27(2):108814
- Nat Commun, 2023, 14(1):4761
- Nat Commun, 2023, 14(1):4761
|
|
S2239 |
Tubacin
|
Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1. Tubacin reduces the replication of the Japanese Encephalitis Virus via the decrease of viral RNA synthesis. |
- Dev Cell, 2024, S1534-5807(24)00326-5
- Br J Cancer, 2023, 10.1038/s41416-023-02195-0
- Int J Mol Sci, 2023, 24(5)4720
|
|
S1156 |
Capecitabine
|
Capecitabine is a tumor-selective fluoropyrimidine carbamate, which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU. Capecitabine treatment of HCT-15 cells causes condensation of DNA and induces apoptosis. |
- Genes Dis, 2024, 11(1):430-448
- Naunyn Schmiedebergs Arch Pharmacol, 2024, 10.1007/s00210-024-03145-0
- J Pers Med, 2022, 12(2)258
|
|
S5971 |
Pemetrexed
|
Pemetrexed (LY231514) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis. |
- Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887
- Cell Rep Med, 2024, 5(7):101615
- Mol Cancer Res, 2024, 22(1):82-93
|
|
S1373 |
Daptomycin
|
Daptomycin is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms. |
- Molecules, 2023, 28(2)621
- Infect Drug Resist, 2023, 16:4867-4879
- Infect Drug Resist, 2023, 16:4867-4879
|
|
S1199 |
Cladribine
|
Cladribine is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively. |
- Oncotarget, 2024, 15:220-231
- Exp Hematol Oncol, 2023, 12(1):23
- Neurol Neuroimmunol Neuroinflamm, 2023, 10(5)e200149
|
|
S7419 |
Blasticidin S HCl
|
Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes. It acts by blocking hydrolysis of peptidyl-tRNA induced by release factors and inhibits peptide bond formation. It is used to select transfected cells carrying bsr or BSD resistance genes. |
- Nucleic Acids Res, 2024, gkae787
- Cell Rep Med, 2024, 5(5):101533
- Pharmacol Res, 2024, 206:107283
|
|
S5582 |
Cytarabine hydrochloride
|
Cytarabine is a pyrimidine nucleoside analog that is used mainly in the treatment of leukemia. It is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. |
- Blood, 2022, blood.2022016090
- Clin Transl Med, 2022, 12(2):e722
- Front Pharmacol, 2022, 13:1032975
|
|
S7975 |
Favipiravir (T-705)
|
Favipiravir (T-705) is a potent and selective RNA-dependent RNA polymerase inhibitor, used to treat influenza virus infections.
|
- J Med Virol, 2024, 96(1):e29372
- Okayama University, 2023 , 10.18926/65391
- Nat Commun, 2022, 13(1):2256
|
|
S1218 |
Clofarabine
|
Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis. |
- Front Oncol, 2023, 13:1287444
- Cancer Res, 2022, 82(4):721-733
- Clin Transl Med, 2022, 12(2):e747
|
|
S8246 |
RK-33
|
RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells. |
- Cell Rep, 2024, 43(3):113937
- JCI Insight, 2023, 8(7)e167566
- Mol Immunol, 2023, 154:54-60
|
|
S1302 |
Ifosfamide
|
Ifosfamide is a nitrogen mustard alkylating agent used in the treatment of cancer. |
- Cancer Res, 2023, 83(16):2750-2762
- Comput Struct Biotechnol J, 2023, 21:3827-3840
- Comput Struct Biotechnol J, 2023, 21:3827-3840
|
|
S1807 |
Acyclovir (Aciclovir)
|
Acyclovir (Aciclovir) is a synthetic nucleoside analogue active against herpesviruses. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells. |
- Cell, 2023, 186(14):3033-3048.e20
- iScience, 2022, 25(12):105682
- Pharmaceutics, 2022, 14(3)536
|
|
S1289 |
Carmofur
|
Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer. |
- JCI Insight, 2023, 8(9)e166850
- Cell Death Discov, 2023, 9(1):451
- Int J Mol Sci, 2023, 24(7)6062
|
|
S7470 |
Triapine (3-AP)
|
Triapine (3-AP) is a potent ribonucleotide reductase (RNR) inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2. |
- J Virol, 2023, 97(8):e0026723
- Res Sq, 2023, rs.3.rs-3126261
- Cancer Res, 2022, 82(4):721-733
|
|
S1192 |
Raltitrexed
|
Raltitrexed (ZD-1694) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth. |
- Mol Ther, 2022, S1525-0016(22)00717-1
- ACS Chem Neurosci, 2022, 13(17):2646-2657
- Biochem Biophys Res Commun, 2022, 610:1-7
|
|
S1221 |
Dacarbazine
|
Dacarbazine is a triazene derivative with antineoplastic activity. Dacarbazine alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis; used in the treatment of various cancers. |
- Cell Death Dis, 2023, 14(6):348
- BMC Complement Med Ther, 2023, 23(1):111
- BMC Complement Med Ther, 2023, 23(1):111
|
|
S1305 |
Mercaptopurine (6-MP)
|
Mercaptopurine(6-MP) is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA. |
- Nat Commun, 2023, 14(1):5913
- Nat Commun, 2023, 14(1):5913
- J Pers Med, 2022, 12(2)258
|
|
S8434 |
B02
|
B02 is a small-molecule inhibitor of human RAD51 with an IC50 of 27.4 μM, but does not inhibit its E. coli homologue RecA (IC50 > 250 μM). |
- iScience, 2024, 27(2):108814
- Cell Prolif, 2023, 56(4):e13384
- Cancer Med, 2023, 12(6):6594-6602
|
|
S7718 |
BMH-21
|
BMH-21 is a DNA intercalator, which binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription.
|
- Nucleic Acids Res, 2024, gkae316
- Elife, 2024, 13e80684
- J Biol Chem, 2024, 300(3):107115
|
|
S1213 |
Nelarabine
|
Nelarabine (506U78,Arranon) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells. |
- Cancer Res, 2022, 82(4):721-733
- Cell Rep, 2022, 39(10):110913
- J Pers Med, 2022, 12(2)258
|
|
S7679 |
YK-4-279
|
YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).
|
- Nat Commun, 2024, 15(1):4590
- Cancers -Basel), 2023, 15(19)4772
- Cell Chem Biol, 2022, 29(8):1325-1332.e4
|
|
S1764 |
Rifampin (Rifampicin)
|
Rifampin (Rifampicin) is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections. |
- Cell Death Dis, 2023, 14(1):64
- Int J Mol Sci, 2022, 23(13)7383
- Biomedicines, 2021, 9(8)996
|
|
S1299 |
Floxuridine (FUDR)
|
Floxuridine (FUDR) is a prodrug that is rapidly catabolized to 5-fluorouracil in vivo. Floxuridine is used to treat various cancers, particularly metastases to the liver. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage and apoptosis. Floxuridine has antiviral effects against HSV and CMV. |
- J Pers Med, 2022, 12(2)258
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Cell Chem Biol, 2021, S2451-9456(21)00306-8
|
|
S1949 |
Menadione (Vitamin K3)
|
Menadione (Vitamin K3), a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement. |
- Med -N Y, 2022, S2666-6340-2200365-8
- Mol Cell, 2021, S1097-2765(21)00269-0
- DNA Repair (Amst), 2021, 105:103152
|
|
S1995 |
Procarbazine HCl
|
Procarbazine HCl (NSC-77213) is a hydrochloride salt form of procarbazine which is a polyfunctional alkylating compound, used for the treatment of Hodgkin's lymphoma. |
- J Pers Med, 2022, 12(2)258
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 34(6):1911-1918
|
|
S4239 |
Bergapten
|
Bergapten is a psoralen that can be photoactivated and is capable of crossing-linking DNA, covalently modifying proteins and lipids, and consequently inhibiting cell replication. |
- J Pers Med, 2022, 12(2)258
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 10.1007/s13577-021-00579-z
|
|
S4288 |
Chloroambucil
|
Chloroambucil (Chlorambucil,CB-1348,WR-139013) is a nitrogen mustard alkylating agent, used in the treatment of chronic lymphocytic leukemia.
|
- bioRxiv, 2023, 2023.01.17.524444
- J Pers Med, 2022, 12(2)258
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S1516 |
Cidofovir
|
Cidofovir suppresses virus replication by selective inhibition of viral DNA synthesis. |
- Oncol Lett, 2021, 21(4):280
- Nat Biotechnol, 2019, 37(3):303-313
- Antiviral Res, 2019, 162:178-185
|
|
S2678 |
NSC 207895
|
NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase. |
- PLoS One, 2024, 19(1):e0295629
- Front Oncol, 2021, 11:582511
- Genes Dev, 2020, 34(7-8):526-543
|
|
S1778 |
Trifluridine (NSC 75520)
|
Trifluridine (NSC 529182, NSC 75520, Viroptic, Trifluorothymidine, TFT) is an anti-herpesvirus antiviral agent by interacting viral DNA replication, used primarily on the eye. |
- Nat Med, 2023, 29(3):605-614
- JCI Insight, 2022, 7(22e158060)
- Biochem Biophys Res Commun, 2022, 610:119-126
|
|
S1300 |
Tegafur (FT-207)
|
Tegafur (NSC 148958,Fluorafur,FT-207) is a substance being used in the treatment of some types of cancer. |
- J Pers Med, 2022, 12(2)258
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 34(6):1911-1918
|
|
S8144 |
Halofuginone
|
Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal. |
- Cell Rep, 2024, 43(9):114728
- J Neurochem, 2024, 10.1111/jnc.16102
- Infect Agent Cancer, 2023, 18(1):27
|
|
S4227 |
Fidaxomicin
|
Fidaxomicin is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit. |
- J Antimicrob Chemother, 2024, dkae101
- Nucleic Acids Res, 2023, 51(19):e99
- bioRxiv, 2023, 2023.03.13.532464
|
|
S1384 |
Mizoribine
|
Mizoribine is an imidazole nucleoside and an immunosuppressant that inhibits HCV RNA replication with IC50 of ~ 100 μM for anti-HCV activity. Mizoribine is a selective inhibitor of inosine-5'-monophosphate dehydrogenase (IMPDH) and guanosine monophosphate synthetase. Mizoribine also inhibits SARS-CoV. |
- EMBO J, 2023, e110620.
- bioRxiv, 2022, 2021.07.02.450964
- Cell Death Differ, 2021, 10.1038/s41418-021-00853-5
|
|
S4297 |
Mupirocin
|
Mupirocin(BRL-4910A,Pseudomonic acid) is an isoleucyl t-RNA synthetase inhibitor, used in the treatment of bacterial skin infections.
|
- Infect Drug Resist, 2023, 16:4867-4879
- Infect Drug Resist, 2023, 16:4867-4879
- Anaerobe, 2020, 62:102169
|
|
S1217 |
Cyclophosphamide
|
Cyclophosphamide(NSC 26271,Endoxan, Cytoxan, Neosar, Procytox, Revimmune, Cytophosphane) is a nitrogen mustard alkylating agent from the oxazophorines group. |
- J Immunother, 2024, 10.1097/CJI.0000000000000505
- Oncol Lett, 2024, 27(4):158
- Stem Cell Res Ther, 2023, 14(1):75
|
|
S1973 |
Cyclocytidine HCl
|
Cyclocytidine (NSC 145668) is the prodrug of cytarabine, which is a pyrimidine nucleoside analog that inhibits the DNA synthesis and used mainly in the treatment of leukemia. |
- Transl Oncol, 2023, 35:101712
- PeerJ, 2022, 10:e13719
- Acta Biochim Biophys Sin (Shanghai), 2020, 14 pii: gmaa017
|
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S5948 |
Amodiaquine
|
Amodiaquine is a synthetic aminoquinoline that acts by binding to the protozoal or parasitic DNA and preventing DNA and RNA production and subsequent protein synthesis. It is used for the therapy of malaria. |
- Molecules, 2024, 29(6)1363
- Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
- bioRxiv, 2020, 10.1101/2020.04.13.039917
|
|
S1907 |
Metronidazole
|
Metronidazole, a synthetic antibacterial and antiprotozoal agent of the nitroimidazole class, is used against protozoa. |
- Microorganisms, 2022, 10(7)1421
- Elife, 2021, 10e69795
- Bone Joint Res, 2020, 16;9(4):152-161
|
|
S1760 |
Rifapentine
|
Rifapentine (MDL473) is an antibiotic, which inhibits DNA-dependent RNA polymerase activity, used to treat tuberculosis. |
- Int J Mol Sci, 2022, 23(13)7383
- Front Microbiol, 2020, 10:2936
- mSphere, 2018, 3(5)
|
|
S1784 |
Vidarabine
|
Vidarabine is an antiviral drug by interfering with the synthesis of viral DNA, used to treat herpes simplex and varicella zoster viruses. |
- Neuron, 2017, 96(6):1290-1302
- ACS Appl Mater Interfaces, 2016, 8(39):25818-25824
- Biogerontology, 2016, 17(5-6):907-920
|
|
S1826 |
Nedaplatin
|
Nedaplatin(NSC 375101D) is a derivative of cisplatin and DNA damage agent for tumor colony forming units with IC50 of 94 μM.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation. |
- Nat Commun, 2019, 10(1):5654
- Cancer Res, 2018, 78(19):5694-5705
- Oncol Lett, 2016, 12(5):4195-4202
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|
S7445 |
APX-3330
|
APX-3330 (E3330) is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.
|
- J Transl Med, 2023, 21(1):183
- Cell Death Dis, 2022, 13(2):124
- Cancer Research on Prevention and Treatment, 2020, (7): 492-497
|
|
S7757 |
6-Thio-dG
|
6-thio-dG (β-TGdR) is a nucleoside analog and telomerase substrate.
|
- Cell Death Discov, 2024, 10(1):381
- Radiation Medicine and Protection, 2022, 64-71
- Clin Sci (Lond), 2020, 10.1042/CS20190890
|
|
S9521 |
Pentostatin
|
Pentostatin(CI-825,Deoxycoformycin) is a potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, particularly hairy-cell leukemia. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity. |
- Res Sq, 2023, rs.3.rs-2276903
- Nat Metab, 2020, 10.1038/s42255-020-0227-4
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|
S8539 |
TAS-102
|
TAS-102 (Trifluridine-Tipiracil Hydrochloride Mixture) is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride. |
- STAR Protoc, 2024, 5(2):103090
- J Exp Clin Cancer Res, 2023, 42(1):8
- Adv Sci (Weinh), 2021, e2103360
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S3669 |
Carmustine
|
Carmustine (bis-chloroethylnitrosourea, BCNU, BiCNU) is a cell-cycle phase nonspecific alkylating antineoplastic agent and used in the treatment of brain tumors and various other malignant neoplasms. |
- Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
- Cancer Res, 2021, 81(23):6044-6057
|
|
S8850 |
JH-RE-06
|
JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS). |
- Nucleic Acids Res, 2024, gkae317
- Nucleic Acids Res, 2024, gkae785
- Cell Rep, 2024, 43(5):114205
|
|
S7546 |
Pritelivir (BAY 57-1293)
|
Pritelivir (BAY 57-1293, AIC316) is a potent helicase primase inhibitor, exhibiting antiviral effect on herpes simplex virus (HSV) with IC50 of 20 nM for both HSV-1 and HSV-2.
|
- PLoS Pathog, 2021, 17(11):e1010117
- J Virol, 2021, JVI0166621
|
|
S9718 |
TK216
|
TK216 is a potent inhibitor targeting E26 transformation specific (ETS) factors via blocking the protein-protein interaction with RNA helicases. TK216 exhibits antilymphoma activity.
|
- J Biol Chem, 2024, 300(6):107375
- Sci Rep, 2023, 13(1):14360
- Sci Rep, 2023, 13(1):14360
|
|
S1790 |
Rifaximin
|
Rifaximin is a RNA synthesis inhibitor by binding the β subunit of the bacterial DNA-dependent RNA polymerase, used to treat traveler's diarrhea caused by certain bacteria. |
- Int J Mol Sci, 2022, 23(13)7383
|
|
S5552 |
Amenamevir
|
Amenamevir (ASP2151) is a potent helicase-primase inhibitor and a novel class of antiviral agent. |
- J Biomol Struct Dyn, 2020, 1-14
|
|
S0280 |
Madrasin
|
Madrasin (DDD00107587) is a potent and cell-penetrant pre-mRNA splicing inhibitor. Madrasin interferes with the early stages of spliceosome assembly and stalls spliceosome assembly at the A complex. |
- Leukemia, 2023, 37(8):1649-1659
|
|
S8095 |
Tubercidin
|
Tubercidin (7-deaza-adenosine), an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities. |
- Mol Cell, 2020, 80(6):1104-1122.e9
|
|
S5484 |
Rimantadine Hydrochloride
|
Rimantadine is an RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. It works by inhibiting a viral protein called M2, which normally mediates the transport of acid ions across the influenza virion shell. |
- bioRxiv, 2020, 2020.08.12.246389
|
|
S3168 |
cis-Resveratrol
|
cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
- J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
|
|
S4737 |
Psoralen
|
Psoralen (Psoralene, Ficusin, Furocoumarin) is a naturally occurring furocoumarin that intercalates with DNA, inhibiting DNA synthesis and cell division. |
- Metabolites, 2022, 13(1)3
|
|
E0488 |
BC-LI-0186
|
BC-LI-0186 is a selective blocker of Leucyl-tRNA synthetase (LRS, LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (LRS-RagD interaction) (IC50 = 46.11 nM) by competing against RagD for LRS VC domain binding (KD = 42.1 nM), thereby inhibiting lysosomal localization of LRS and mTORC1 activity. It also effectively suppresses the activity of cancer-associated mTOR mutants and the growth of rapamycin-resistant cancer cells. |
- Cancer Res Treat, 2023, 55(3):851-864
|
|
S5953 |
Menadione bisulfite sodium
|
Menadione(Vitamin K3) bisulfite sodium, a fat-soluble compound, is an inhibitor of Cdc25 phosphatase and mitochondrial DNA polymerase γ (pol γ), used as a nutritional supplement. |
- Life Sci, 2020, 242:117159
|
|
S7449 |
CRT0044876
|
CRT0044876 (NSC 69877, 7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM. |
- Cell Rep, 2024, 43(10):114820
- Nat Biotechnol, 2017, 35(5):463-474
|
|
S3549 |
PFM01
|
PFM01, a cell-permeable N-alkylated Mirin derivative, is a selective inhibitor of MRE11 endonuclease activity. |
- Cell Rep, 2023, 42(7):112792
|
|
S7637 |
DTP3
|
DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway. |
- Life Sci Alliance, 2024, 7(8)e202302555
- MedComm (2020), 2023, 4(3):e269
|
|
S6854 |
Triazavirin (TZV)
|
Triazavirin (TZV) is a novel antiviral drug, a nucleoside analogue of nucleic acid that inhibits the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is active against influenza and a number of other viruses. Triazavirin is an effective protective agent on the transmission stage of influenza. |
- Nature, 2022, 604(7904):120-126
|
|
S0469 |
ML216
|
ML216 (CID-49852229) is a potent and selective inhibitor of the DNA unwinding activity of BLM(Bloom’s syndrome protein) with antitumor activity. ML216 inhibits helicases with IC50 of 0.97 μM and 2.98 μM for BLM636-1298 and BLMfull-length, respectively. |
- Elife, 2024, 13RP99026
- Cells, 2022, 12(1)145
|
|
S3001 |
Clevudine
|
Clevudine(Levovir,L-FMAU) is an antiviral drug for the treatment of hepatitis B. |
- J Biomed Sci, 2024, 31(1):34
|
|
E2939 |
Didox
|
Didox (3,4-dihydroxy-benzohydroxamic acid) is a synthetic ribonucleotide reductase (RR) inhibitor derived from polyhydroxy-substituted benzohydroxamic acid. Didox inhibits proliferation of resistant breast cancer cells. |
|
|
S3009 |
Menthone
|
Menthone is one of the main volatile components of the essential oil of peppermint (Mentha piperita L.). Menthone is used as antioxidant agent and has a good compensatory effect with significant reduction in DNA damages in sperm cells.
|
|
|
S3472 |
Metarrestin
|
Metarrestin is an orally active and specific perinucleolar compartment (PNC) inhibitor that disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription. Metarrestin blocks metastatic development and extends survival in mouse cancer models. |
|
|
E1152 |
AGX51
|
AGX51, a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader, inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability, also inhibits pathologic ocular neovascularization. |
|
|
S8376 |
Rbin-1
|
Rbin-1 (Ribozinoindole-1) is a potent chemical inhibitor of eukaryotic ribosome assembly. It inhibits recombinant full-length Mdn1's ATPase activity in vitro. |
|
|
E0459 |
Robinetin
|
Robinetin inhibits HIV integrase cleavage and integration in a dose-dependent manne, inhibits the DNA synthesis in Proteus vulgaris, and the RNA synthesis in S. aureus, also inhibits egg yolk phosphatidylcholine (EYPC) membrane lipid peroxidation and hemoglobin A (HbA) glycosylation with high efficiency. |
|
|
E1596 |
AOH1996
|
AOH1996 is an orally active small-molecule PCNA inhibitor with potential anti-tumor activity. It enhances the interaction between PCNA and RPB1, the largest subunit of RNA polymerase II. |
|
|
S0816 |
Brr2 Inhibitor C9
|
Brr2 inhibitor C9 (Brr2 Inhibitor 9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa a group of progressive retinal degenerative disorders. |
|
|
E1528New |
RP-6685
|
RP-6685 is a potent, selective, and orally active inhibitor of DNA polymerase theta (Polθ). RP-6685 exhibits antitumor efficacy in animal models. |
|
|
S9775 |
SCR130
|
SCR130 is a novel DNA repair inhibitor with IC50s of 14 μM in Reh cells and 2 μM in Nalm6 cells. SCR130 specifically inhibits DNA Ligase IV‐mediated joining with minimal or no effect on Ligase III and Ligase I mediated joining. |
|
|
S5813 |
Isoginkgetin
|
Isoginkgetin is a naturally derived biflavonoid with anti-tumor activity. Isoginkgetin directly inhibits the chymotrypsin-like, trypsin-like, and caspase-like activities of the 20S proteasome. Isoginkgetin also is a general inhibitor of Pre-mRNA splicing. |
- Cell Death Dis, 2024, 15(4):289
- Cell Death Dis, 2024, 15(4):289
|
|
S8328 |
CeMMEC1 HCl
|
CeMMEC1 is an N-methylisoquinolinone derivative that inhibits the second bromodomain of TAF1 (IC50=0.9 μM). |
|
|
S0054 |
D-I03
|
D-I03 is a selective inhibitor of RAD52 with Kd of 25.8 µM. D-I03 inhibits ssDNA annealing by RAD52 and D-loop formation with IC50 of 5 µM and 8 µM, respectively. |
|
|
S0063 |
RG3039
|
RG3039 (PF-06687859, PF 6687859, Quinazoline 495) is an orally bioavailable and brain-penetrant inhibitor of the mRNA decapping enzyme DcpS with IC50 of 4.2 nM and IC90 of 40 nM, respectively. |
|
|
S4504 |
6-Mercaptopurine (6-MP) Monohydrate
|
6-Mercaptopurine (6-MP) Monohydrate is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.
|
|
|
S0780 |
Oncrasin-1
|
Oncrasin-1 (Onc-1) is a potent RNA polymerase II inhibitor with antitumor activity that kills various human lung cancer cells with K-Ras mutations. Oncrasin-1 drives abnormal aggregation of protein kinase C iota (PKCι) in nucleus of sensitive cells but not in resistant cells. |
|
|
S8942 |
Suramin sodium salt
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatase (PTPases) inhibitor, also is the potent inhibitor of sirtuins, purified topoisomerase II and SARS-CoV-2 RNA-dependent RNA polymerase (RdRp). |
- J Biol Chem, 2024, S0021-9258(24)00128-5
|
|
S9286 |
Neobavaisoflavone
|
Neobavaisoflavone, isolated from seeds of Psoralea corylifolia, exhibits inhibitory activity against DNA polymerase and platelet aggregation. |
|
|
S6848 |
3'-Fluoro-3'-deoxythymidine (Alovudine)
|
3'-Fluoro-3'-deoxythymidine (Alovudine, CL 184824, FddThd, FLT, MIV-310) is a potent inhibitor of polymerase γ and reverse transcriptase that can be used in the treatment of HIV infection. 3'-Fluoro-3'-deoxythymidine (Alovudine) is also a marker of DNA synthesis that can be used as an early response biomarker in the chemotherapy of pancreatic cancer. |
|
|
E0443 |
LDC195943 (IMT1)
|
LDC195943 (IMT1) is a specific and noncompetitive inhibitor of human mitochondrial RNA polymerase (POLRMT). IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases. |
|
|
E0444 |
LDC203974 (IMT1B)
|
LDC203974 (IMT1B) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. LDC203974 has anti-tumour effects. |
|
|
S8964 |
Actinomycin D (Dactinomycin)
|
Actinomycin D (Dactinomycin, Act D, RASP-101) is a significant polypeptide antibiotic isolated from soil bacteria of the genus Streptomyces. Actinomycin D (Dactinomycin) inhibits DNA repair and rests the cell cycle at G1 phase with IC50 of 0.42 μM and 0.4 nM, respectively. Actinomycin D is an autophagy activator, induces p53-independent cell death and prolongs survival in high-risk chronic lymphocytic leukemia.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing. |
- Mol Cancer, 2024, 23(1):186
- Nat Commun, 2024, 15(1):5209
- Exp Mol Med, 2024, 10.1038/s12276-024-01315-x
|
|
S9649 |
Acelarin (NUC-1031)
|
Acelarin (NUC-1031, CPF-31, MTL-007, GTPL7389) is a DNA synthesis inhibitor with EC50 of 0.2 nM. |
|
|
E1331 |
SU056
|
SU056 is an inhibitor of Y box binding protein 1 (YB-1) with IC50 of 1.73 μM in Sk0V3 cells. |
- Cancer Lett, 2024, 602:217197
- Transl Oncol, 2024, 45:101965
|
|
E1987New |
APX2009
|
APX2009 is a second-generation redox-specific inhibitor of APE1/Ref-1, an essential enzyme in the base excision repair (BER) pathway. APX2009 effectively reduces breast cancer cell proliferation and colony formation. |
|
|
S0102 |
L 189
|
L 189 is a novel human DNA ligase inhibitor with IC50 of 5 μM, 9 μM and 5 μM for hLigI, hLigIII and hLigIV, respectively. L 189 inhibits base excision repair (BER) and non-homologous end joining (NHEJ). L 189 specifically sensitizes cancer cells to DNA damage. |
|
|
S9936 |
ART558
|
ART558 is a potent, selective, low molecular weight, allosteric inhibitor of DNA Polθ with an IC50 of 7.9 nM. |
|
|
S3641 |
Osalmid
|
Osalmid suppresses ribonucleotide reductase (RNR) activity in a concentration-dependent manner, with a 50% RR activity-inhibitory concentration (IC50) of 8.23 μM. |
|
|
S3360 |
Bis(2-ethylhexyl) phthalate
|
Bis(2-ethylhexyl) phthalate (Dioctyl phthalate, DOP, Diplast O, ESBO-D 82, Ergoplast FDO, Ergoplast FDO-S, Etalon) induces DNA strand breaks and gene expression alterations in larval zebrafish Danio rerio. |
|
|
S5293 |
Nimustine Hydrochloride
|
Nimustine Hydrochloride (Nidran) is the hydrochloride salt of nimustine, a nitrosourea with antineoplastic activity that alkylates and crosslinks DNA, thereby causing DNA fragmentation, inhibition of protein synthesis, and cell death. |
|
|
S5297 |
Vidarabine monohydrate
|
Vidarabine (Spongoadenosine, Vira-A) is a nucleoside antibiotic with antiviral acitivity that interferes with the synthesis of viral DNA. It is used to treat herpes simplex and varicella zoster viruses. |
|
|
S1126New |
CX-3543(Quarfloxin)
|
Quarfloxin (CX-3543), a fluoroquinolone derivative inhibits RNA pol I activity. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template. |
|
|
E1111 |
VV116
|
VV116, a promising orally administered anti-SARS-CoV-2 nucleoside drug candidate, exerts functions by targeting the viral RNA-dependent RNA polymerase through its nucleoside triphosphate form with an IC50 of 0.67±0.24 μM. |
|
|
S6115 |
Pyridoxal 5′-phosphate hydrate
|
Pyridoxal 5′-phosphate (pyridoxal phosphate, Vitamin B6 phosphate, PAL-P, PLP), a vitamin B6 phosphate, is a coenzyme in a variety of enzymatic reactions. Pyridoxal 5′-phosphate at concentrations < 0.5 mM inhibits of polymerization deoxynucleoside triphosphate catalysed by variety of DNA polymerases isolated from type C RNA tumor viruses. The combination of Pyridoxal 5′-phosphate and NEIL2 will make NEIL2 completely lose its ability to bind damaged DNA. |
|
|
E2921 |
Diethyl Pyrocarbonate
|
Diethyl pyrocarbonate is a potent, non-specific inhibitor of RNase. It has been useful as an in vitro agent, relatively specific for binding to imidazole of histidine. It inhibits central chemosensitivity in rabbit and can modify Ser, Thr, His and Tyr residues. |
|
|
S3356 |
Phosphonoacetic acid
|
Phosphonoacetic acid (PAA) is an active endogenous metabolite that possesses a restricted potential to block DNA biosynthesis. Phosphonoacetic acid exhibits anti-viral activities. |
|
|
S0161 |
ML367
|
ML367 is a potent, micromolar inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization. ML367 blocks DNA repair pathways and general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation. |
|
|
S8977 |
BCH001
|
BCH001 is a specific PAPD5 inhibitor that restores telomerase activity and telomere length in dyskeratosis congenita (DC) patient induced pluripotent stem cells. PAPD5 is a noncanonical poly(A) polymerase with an unusual RNA-binding motif. |
|
|
E0510 |
Cidofovir hydrate
|
Cidofovir hydrate is a selective inhibitor of viral DNA synthesis through the selective inhibition of viral DNA polymerase. |
|
|
E1529 |
ART812
|
ART812 is an orally active DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. |
|
|
S4236 |
Proflavine Hemisulfate
|
Proflavine Hemisulfate is a topical antiseptic by interchelating DNA, thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands. |
|
|
S2600 |
Fexinidazole
|
Fexinidazole (HOE-239, Fexinidazole Winthrop) is a 5-nitroimidazole derivative. Fexinidazole is a DNA synthesis inhibitor and the only, all-oral agent for Human African Trypanosomiasis(HAT or sleeping sickness). |
- Int J Mol Sci, 2024, 25(8)4413
|
|
S2961 |
GC7 Sulfate
|
GC7 (N1-guanyl-1,7-diaminoheptane) Sulfate is an inhibitor of deoxyhypusine synthase (DHPS). GC7 inhibits Neuroblastoma (NB) cell proliferation in a dose-dependent manner, through induction of the cell cycle inhibitor p21 and reduction of total and phosphorylated Rb proteins. |
- Exp Mol Med, 2024, 10.1038/s12276-024-01214-1
|
|
S4782 |
5-methoxyflavone
|
5-methoxyflavone is a novel DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. |
|
|
S4537 |
Oxolinic acid
|
Oxolinic acid (Urinox, NSC 110364) is a quinolone antibiotic, inhibiting the enzyme DNA gyrase and DNA synthesis.It also acts as a dopamine reuptake inhibitor. |
|
|
E1070 |
Phen-DC3 Trifluoromethanesulfonate
|
Phen-DC3 Trifluoromethanesulfonate is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65 ± 6 and 50 ± 10 nM, respectively. |
|
|
S8329 |
CeMMEC13
|
CeMMEC13 is an isoquinolinone that selectively inhibits the second bromodomain of TAF1 (IC50 = 2.1 µM). |
|
|
E0511 |
Framycetin sulphate
|
Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM, and competes for specific divalent metal ion binding sites in RNase P RNA, also inhibits hammerhead ribozyme with a Ki of 13.5 μM. |
|
|
S2427 |
Triglycidyl Isocyanurate (Teroxirone)
|
Triglycidyl Isocyanurate (Teroxirone, Tris(2,3-epoxypropyl) Isocyanurate, TGI, TGIC) is a triazene triepoxide with antineoplastic activity. It inhibits growth of human non-small cell lung cancer cells by activating p53. Triglycidyl Isocyanurate alkylates and cross-links DNA, thereby inhibiting DNA replication. Triglycidyl Isocyanurate is also used in various polyester powder coatings in the metal finishing industry. |
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