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P450 (e.g. CYP17) Signaling Pathway

P450 (e.g. CYP17) Products

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  • New P450 (e.g. CYP17) Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1185 Ritonavir Ritonavir is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.
Cell Chem Biol, 2024, S2451-9456(24)00396-9
Antiviral Res, 2024, 225:105840
Cancer Drug Resist, 2024, 7:3
S2476 Itraconazole Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Cell Infect Microbiol, 2023, 13:1131641
Front Cell Infect Microbiol, 2022, 12:864912
S1123 Abiraterone Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.
Cancer Res, 2023, 83(8):1361-1380
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancers (Basel), 2021, 13(16)3959
S2246 Abiraterone Acetate Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay. Abiraterone acetate is an oral androgen biosynthesis inhibitor.
Cells, 2024, 13(19)1622
Cancer Res, 2023, 83(2):219-238
J Immunother Cancer, 2023, 11(5)e006581
S2262 Apigenin Apigenin is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.
Antioxidants (Basel), 2024, 13(5)611
bioRxiv, 2024, 2024.04.04.588167
bioRxiv, 2024, 2024.04.04.588167
S2268 Baicalein Baicalein is a CYP2C9 and prolyl endopeptidase inhibitor.
SLAS Discov, 2024, S2472-5552(24)00007-8
Redox Rep, 2023, 28(1):2152607
Microbiol Spectr, 2023, 11(3):e0470222
S1257 Posaconazole Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.
Front Cell Infect Microbiol, 2023, 13:1131641
Front Cell Infect Microbiol, 2022, 12:1074903
Front Cell Infect Microbiol, 2022, 12:864912
S1442 Voriconazole Voriconazole is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol.
Pharmaceutics, 2024, 16(7)897
Front Cell Infect Microbiol, 2023, 13:1131641
Front Cell Infect Microbiol, 2022, 12:864912
S1331 Fluconazole Fluconazole is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.
Front Cell Infect Microbiol, 2024, 14:1296151
Front Cell Infect Microbiol, 2023, 13:1131641
Nat Commun, 2022, 13(1):1658
S1353 Ketoconazole Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor.
J Med Virol, 2023, 95(6):e28856
J Med Virol, 2023, 95(6):e28856
Cell Death Dis, 2023, 14(1):64
S4202 Verapamil HCl Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.
NPJ Precis Oncol, 2024, 8(1):94
Int J Mol Sci, 2024, 25(18)10162
Biomedicines, 2024, 12(4)904
S2187 Avasimibe Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.
Nat Commun, 2024, 15(1):8301
PLoS Pathog, 2023, 19(5):e1011323
Hepatol Int, 2023, 10.1007/s12072-023-10490-4
S1712 Deferasirox Deferasirox is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death.
Elife, 2023, 12RP88745
J Transl Med, 2023, 21(1):50
Cell Death Discov, 2023, 9(1):97
S1794 Fenofibrate Fenofibrate is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.
Heliyon, 2024, 10(11):e31861
Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
Cell Metab, 2022, 34(2):299-316.e6
S2900 Cobicistat Cobicistat is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S2046 Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.
J Transl Med, 2024, 22(1):593
Commun Biol, 2022, 5(1):231
J Genet Genomics, 2022, S1673-8527(22)00133-3
S2394 Naringenin Naringenin (NSC 34875, S-Dihydrogenistein, NSC 11855, Salipurol) is a natural predominant flavanone derived from plant food, which is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.
J Transl Med, 2024, 22(1):208
J Lipid Res, 2024, S0022-2275(24)00044-0
Molecules, 2023, 28(13)4947
S4662 Atazanavir Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.
Int J Mol Sci, 2022, 23(23)15380
Chemistry, 2022, e202202798.
Sci Rep, 2021, 11(1):19443
S1952 Methoxsalen Methoxsalen (Xanthotoxin, NCI-C55903) is a naturally occurring photoactive substance found in the seeds of the Ammi majus (Umbelliferae) plant, used in the diagnosis and treatment of psoriasis; A CYP2A5/6 inhibitor.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S2803 Galeterone Galeterone (TOK-001) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.
ChemMedChem, 2022, e202200043
Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w
Steroids, 2020, 153:108534
S2555 Clarithromycin Clarithromycin (A-56268) is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.
Microorganisms, 2022, 10(7)1421
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09646-5
J Ovarian Res, 2019, 12(1):107
S5658 Omeprazole Sodium Omeprazole Sodium is the sodium salt form of omeprazole, which is a proton pump inhibitor and suppresses gastric acid secretion. Omeprazole Sodium is a metabolism-dependent inhibitor (MDI) of CYP2C19.
Theranostics, 2021, 11(5):2364-2380
Theranostics, 2021, 11(5):2364-2380
J Virol, 2021, JVI.00190-21
S2380 Diosmetin Diosmetin (Luteolin 4-methyl ether) is a bioflavonoid found in spearmint, oregano, and many other plants.
Mol Med Rep, 2020, 22(2):1335-1341
J Med Virol, 2019, 91(8):1440-1447
Int J Biol Sci, 2019, 15(11):2497-2508
S2526 Alizarin Alizarin is a red coloring mordant dye extracted from the roots of madder plants (Rubia tinctorum L). Alizarin strongly inhibits P450 isoform CYP1A1, CYP1A2, and CYP1B1 with IC50 of 6.2 μM, 10.0 μM, and 2.7 μM, respectively in an enzymatic assay. There are also literature reports Alizarin increases the CYP1A1 enzymatic activity and acts as an agonist to the AHR receptor in HepG2 cells.
Chem Res Toxicol, 2023, 36(8):1361-1373
BMC Med, 2022, 20(1):365
Cell Rep, 2020, 14;31(2):107518
S7456 Osilodrostat (LCI699) LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis.
Cells, 2022, 11(21)3344
Drug Metab Dispos, 2022, 50(2):114-127
J Inorg Biochem, 2022, 235:111934
S1195 Orteronel Orteronel(TAK-700) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). TAK-700 (Orteronel) is an androgen biosynthesis inhibitor. Phase 3.
Toxicol Appl Pharmacol, 2023, 475:116638
Drug Metab Dispos, 2017, 45(6):635-645
Biochem Biophys Res Commun, 2016, 477(4):1005-10
S2401 Sodium Danshensu Sodium Danshensu is a mono sodium of danshensu, which is a natural phenolic acid of caffeic acid derivatives isolated from Salvia miltiorrhiza.
Molecules, 2023, 28(4)1551
Front Pharmacol, 2022, 13:946668
Front Pharmacol, 2022, 13:946668
S3931 Ginsenoside Rd Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Drug Des Devel Ther, 2022, 16:2767-2782
J Ginseng Res, 2022, 46(5):700-709
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3874 Curcumenol Curcumenol, a sesquiterpene isolated from Curcuma zedoaria, is known to possess a variety of health and medicinal values which includes neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. It inhibits NF-κB activation by suppressing the nuclear translocation of the NF-κB p65 subunit and blocking IκBα phosphorylation and degradation.
Front Pharmacol, 2022, 13:905966
J Bone Miner Res, 2021, 10.1002/jbmr.4328
Int J Mol Med, 2021, 48(4)192
S5266 Stiripentol Stiripentol (BCX2600) is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.
Cell Metab, 2022, 34(1):90-105.e7
Front Pharmacol, 2021, 12:785586
S6868 Alflutinib (Furmonertinib) mesylate Alflutinib (Furmonertinib) mesylate is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Alflutinib (AST2818), primarily metabolized by CYP3A4, is also a potent CYP3A4 inducer with EC50 of 0.25 μM.
Biomedicines, 2024, 12(7)1412
Int J Mol Sci, 2023, 24(18)13972
Int J Mol Sci, 2023, 24(18)13972
S3833 Amentoflavone Amentoflavone (Didemethyl Ginkgetin) is a biflavonoid originally isolated from Selaginella with antibacterial, antioxidant, antiviral, antidiabetic, and neuroprotective activities.
Front Plant Sci, 2021, 12:740923
Viruses, 2019, 11(5)E466
S5967 Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Front Biosci (Landmark Ed), 2022, 27(8):242
Front Pharmacol, 2021, 12:632201
S3673 Sulfaphenazole Sulfaphenazole (Depocid, Depotsulfonamide, Plisulfan, Raziosulfa) is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).
UNIVERSITY OF APPLIED SCIENCES, 2023,
Chem Biol Interact, 2022, 353:109801
Chem Biol Interact, 2022, 365:110070
S3917 Tetrahydrocurcumin Tetrahydrocurcumin (Tetrahydrodiferuloylmethane, Tetrahydro Curcumin), a major metabolite of curcumin, possesses strong antioxidant and cardioprotective properties. Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit CYP2C9 and CYP3A4.
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
Invest Ophthalmol Vis Sci, 2022, 63(6):26
S3660 Uniconazole (S 3307D) Uniconazole (S 3307D, XE 1019D) is a well known inhibitor of cytochrome P450 monooxygenase that prevents the biosynthesis of trans-zeatin. Uniconazole targets CYP735As with Ki of 22 μM.
Nat Microbiol, 2022, 10.1038/s41564-022-01072-5
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
S2329 Naringin Naringin (Naringoside) is a flavanone glycoside, which exerts a variety of pharmacological effects such as antioxidant activity, blood lipid lowering, anticancer activity, and inhibition of cytochrome P450 enzymes.
Am J Transl Res, 2021, 13(6):6330-6341
Int J Mol Sci, 2020, 21(14):5025
S5416 Metyrapone Metyrapone (NSC-25265, SU-4885) is an inhibitor of the enzyme steroid 11-beta-monooxygenase (CYP11B1) that inhibits adrenal steroid synthesis.
Cells, 2022, 11(21)3344
S6790 Ellipticine hydrochloride Ellipticine Hydrochloride (NSC 71795, PZE) is a potent inhibitor of DNA topoisomerase II and forms covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine Hydrochloride is a natural product isolated from the Australian evergreen tree of the Apocynaceae family with antineoplastic activity.
Viruses, 2022, 15(1)105
S3766 Tanshinone IIA sulfonate sodium Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
J Inflamm Res, 2022, 15:6293-6306
S4221 Benzbromarone Benzbromarone(Desuric) is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.
Hum Mol Genet, 2020, ddaa244
S2344 Piperine Piperine (1-Piperoylpiperidine) is the alkaloid responsible for the pungency of black pepper and long pepper, which has also been used in some forms of traditional medicine and as an insecticide.
Int J Mol Med, 2015, 36(5):1369-76
S2496 Ozagrel Ozagrel (OKY-046) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
S1739 Thiabendazole Thiabendazole inhibits the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property, used as an anthelmintic and fungicide agent. It is a potent inhibitor of cytochrome P450 1A2 (CYP1A2).
S2067 Ozagrel HCl Ozagrel HCl (OKY-046) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
S4155 Chlorzoxazone Chlorzoxazone(Chlorzoxazon,Paraflex) is a muscle-relaxing drug,and a probe for human liver cytochrome P-450IIE1.
S5169 2,6-Dihydroxyanthraquinone 2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity.
S0721 Ticlopidine Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina,PCR 5332) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP). Ticlopidine is also an inhibitor of CYP2B6 with Ki of 0.2 μM.
S0922 Salvianolic acid C Salvianolic acid C is a non-competitive Cytochrome P4502C8 (CYP2C8) inhibitor and a moderate mixed inhibitor of Cytochrome P45022J2 (CYP2J2).
S2921 PF-4981517 PF-4981517 (CYP3cide, PF-04981517) is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.
S3273 Hypericin Hypericin (Hyp, HY) is a naturally occurring substance found in the common St. John's Wort (Hypericum species) with antidepressive, antineoplastic and antiviral (human immunodeficiency and hepatitis C virus) activities. Hypericin has inhibitory effects on MAO (monoaminoxidase), PKC (protein kinase C), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450).
Eur J Pharmacol, 2021, 900:174071
S3291 Myristicin Myristicin (Myristicine), a terpene-like active component in Nutmeg which is the seed of Myristica fragrans, is a weak inhibitor of monamine oxidase (MAO) and a mechanism-based inhibitor of CYP1A2.
S5252 Ozagrel sodium Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties.
E1650 Opevesostat (ODM208) Opevesostat (ODM208) is the first-in-class, selective, nonsteroidal, oral CYP11A1 inhibitor. ODM208 exhibits a rapid, complete, durable, and reversible inhibition of the steroid hormone biosynthesis in an adrenocortical carcinoma cell model in vitro, in adult noncastrated male mice and dogs, and in patients with CRPC.
S0541 Dazoxiben hydrochloride Dazoxiben hydrochloride (HCl) is a potent, selevtive and orally active inhibitor of thromboxane (TX) synthase. Dazoxiben inhibits TXB2 production in clotting human whole blood with IC50 of 0.3 μM and causes parallel enhancement of PGE2 production.
S9250 Isosilybin Isosilybin (Silymarin, Isosilybinin, Q-100795) is a flavanolignan found in the extract of S. marianum fruits with antioxidant and anticancer activities. Isosilybin inhibits CYP3A4 induction with an IC50 of 74 μM.
S6606 CDD3505 CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
S9257 Acetylshikonin Acetylshikonin is a biologically active compound with anti-cancer and anti-inflammatory activity, which is isolated from the roots of Lithospermum erythrorhizoma. It is a novel general P450 inhibitor with IC50 values of 1.4-4.0 μM for all tested P450s.
E0214 Pachymic acid Pachymic acid(3-O-Acetyltumulosic acid) inhibits the activity of CYP2C9 with the IC50 of 21.25 µM.
S4938 Cedrol Cedrol, a natural occuring sesquiterpene alcohol, is a potent competitive inhibitor of CYP2B6-mediated bupropion hydroxylase with inhibition constant (Ki) value of 0.9 μM. It also inhibits CYP3A4-mediated midazolam hydroxylation with a Ki value of 3.4 μM while only weakly inhibits CYP2C8, CYP2C9, and CYP2C19 activities.
S2389 Naringin Dihydrochalcone Naringin Dihydrochalcone(Naringin DC) is a new-style sweetening agent and an artificial sweetener derived from naringin and also an inhibitor of CYP enzymes.
S4741 Danshensu Danshensu (Salvianic acid A), a herbal preparation used in traditional Chinese medicine, possesses potential antitumor and anti‑angiogenesis effects. Danshensu inhibits CYP2E1 and CYP2C9 with IC50 of 36.63 and 75.76 μm, respectively.
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
E4855New Sertaconazole Sertaconazole(FI-7045) is an imidazole-type antifungal agent that inhibits ergosterol biosynthesis by inhibiting the cytochrome P450-dependent 14α-lanosterol demethylase or Erg11p. This inhibition disrupts fungal cell membrane integrity, ultimately leading to fungal cell death. Sertaconazole is used in the topical treatment of superficial mycoses.
S9299 Ginsenoside F1 Ginsenoside F1, a pharmaceutical component of ginseng, is known to have antiaging, antioxidant, anticancer, and keratinocyte protective effects. Ginsenoside F1 exhibits competitive inhibition of the activity of CYP3A4 with Ki values of 67.8 ± 16.2 μM. Ginsenoside F1 also exhibited a weaker inhibition of the activity of CYP2D6.
S4963 Purpurin Purpurin (1,2,4-Trihydroxyanthraquinone, Hydroxylizaric acid, Verantin) is one of the natural colorants extracted from madder roots and other Rubiaceae family plants. It exhibits anti-angiogenic, antifungal, antibiotic, and antioxidative activities. Purpurin strongly inhibits the activities of CYP1A1, CYP1A2 and CYP1B1.
E0531 TMS TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive human cytochrome P450s B1 (CYP1B1) inhibitor with an IC50 of 6 nM.
S3777 Gentiopicroside Gentiopicroside (GE, Gentiopicrin), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.
S0110 APD597 APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
S5969 Dicloxacillin Sodium hydrate Dicloxacillin Sodium hydrate (DLX, Dycill, Dynapen, Pathocil), a narrow-spectrum β-Lactam antibiotic of the penicillin class, induces drug-metabolizing CYP enzymes to a clinically relevant extent.
S4831 Piperonyl butoxide Piperonyl butoxide (PBO, Butacide, Ethanol butoxide, Pyrenone 606,ENT-14250) is a man-made pesticide synergist, working with insect killers to increase their effectiveness.Piperonyl butoxide is an inhibitor of cytochrome P450 monooxygenases(P450s).
E1830New Baxdrostat Baxdrostat(CIN-107) is a selective and potent inhibitor of aldosterone synthase(CYP11B2), a rate-limiting enzyme in the pathway of aldosterone synthesis, with the potential to treat resistant hypertension. It also inhibits the function of multidrug and toxin extrusion 1 (MATE1) and MATE2-K with IC50 values of 1.34 µM and 2.67 µM, respectively.
E2912 MEHP MEHP (Phthalic acid mono-2-ethylexyl ester) is a competitive inhibitor of CYP2C9 with IC50 of 6.37 μM.
S0175 DMU2105 DMU2105 is a potent and specific inhibitor of CYP1B1 with IC50 of 10 nM.
S0176 DMU2139 DMU2139 is a potent and specific inhibitor of CYP1B1 with IC50 of 9 nM.
S0418 Ezutromid Ezutromid (SMT C1100,BMN 195,VOX-C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM which can be used for the research Duchenne muscular dystrophy (DMD), also inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM.
S3719 Topiroxostat Topiroxostat is a xanthine oxidoreductase (XOR) inhibitor and used for treatment of gout and hyperuricemia. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment.
S2571New Quinidine Quinidine is a pharmaceutical agent that acts as a class I antiarrhythmic agent.
S6886 1-Aminobenzotriazole 1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) is a nonselective and irreversible inhibitor of cytochrome P450 (CYP) enzymes. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT).
S9442 Bergaptol Bergaptol (5-Hydroxypsoralen, 5-Hydroxyfuranocoumarin) is a natural furanocoumarin found in the essential oils of citrus including lemon and bergamot.Bergaptol is a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 μM.
Molecules, 2024, 29(3)713
S5380 7-Hydroxyflavone 7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines.
S5529 Galangin Galangin (3,5,7-trihydroxyflavone; Norizalpinin), a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.
S4784 Phloracetophenone Phloracetophenone, or 2,4,6-trihydroxyacetophenone (THA), the aglycone component of phloracetophenone glucoside, is a naturally occurring compound obtained from the rhizome of Curcuma comosa (Family Zingiberaceae). Phloracetophenone can stimulate CYP7A1 activity. Phloracetophenone induces cholestasis in rats mediated through Mrp2.
S9241 Polygalaxanthone III Polygalaxanthone III is a natural product with the efficacy of tranquilization, glaangal, eliminating sputum and detumescence. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.
S6594 Liarozole dihydrochloride Liarozole Dihydrochloride is identified as a modest inhibitor of P450 with IC50 of 2.2–6.0 μM and 260 nM for CYP26 and rat CYP17 respectively.
S9163 Rhapontigenin Rhapontigenin (Protigenin), produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM).
S0230 NVP-VID-400 NVP-VID-400 (SDZ285428) is an inhibitor of CYP51. NVP-VID-400 (SDZ285428) inhibits T. cruzi and T. brucei with I/E2a(5 min) of both <1 and I/E2(60 min) of 9 and 35, respectively.
S3227 5,7-Dimethoxyflavone 5,7-Dimethoxyflavone (5,7-DMF) is an inhibitor of cytochrome P450 (CYP) 3As that markedly decreases the expression of CYP3A11 and CYP3A25 in the liver. 5,7-Dimethoxyflavone (5,7-DMF) is also a potent Breast Cancer Resistance Protein (BCRP, ABCG2) inhibitor. 5,7-Dimethoxyflavone (5,7-DMF) is one of the major components of Kaempferia parviflora with anti-obesity, anti-inflammatory, and antineoplastic effects.
S6437 Oxolamine Citrate Oxolamine (SKF-9976, AF-438) citrate, a cough suppressant, is an inhibitor of CYP2B1/2. Oxolamine citrate also exhibits anti-inflammatory effect.
S1185 Ritonavir Ritonavir is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.
Cell Chem Biol, 2024, S2451-9456(24)00396-9
Antiviral Res, 2024, 225:105840
Cancer Drug Resist, 2024, 7:3
S2476 Itraconazole Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Cell Infect Microbiol, 2023, 13:1131641
Front Cell Infect Microbiol, 2022, 12:864912
S1123 Abiraterone Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.
Cancer Res, 2023, 83(8):1361-1380
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancers (Basel), 2021, 13(16)3959
S2246 Abiraterone Acetate Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay. Abiraterone acetate is an oral androgen biosynthesis inhibitor.
Cells, 2024, 13(19)1622
Cancer Res, 2023, 83(2):219-238
J Immunother Cancer, 2023, 11(5)e006581
S2262 Apigenin Apigenin is a potent P450 inhibitor for CYP2C9 with Ki of 2 μM.
Antioxidants (Basel), 2024, 13(5)611
bioRxiv, 2024, 2024.04.04.588167
bioRxiv, 2024, 2024.04.04.588167
S2268 Baicalein Baicalein is a CYP2C9 and prolyl endopeptidase inhibitor.
SLAS Discov, 2024, S2472-5552(24)00007-8
Redox Rep, 2023, 28(1):2152607
Microbiol Spectr, 2023, 11(3):e0470222
S1257 Posaconazole Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14ɑ demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours.
Front Cell Infect Microbiol, 2023, 13:1131641
Front Cell Infect Microbiol, 2022, 12:1074903
Front Cell Infect Microbiol, 2022, 12:864912
S1331 Fluconazole Fluconazole is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.
Front Cell Infect Microbiol, 2024, 14:1296151
Front Cell Infect Microbiol, 2023, 13:1131641
Nat Commun, 2022, 13(1):1658
S1353 Ketoconazole Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor.
J Med Virol, 2023, 95(6):e28856
J Med Virol, 2023, 95(6):e28856
Cell Death Dis, 2023, 14(1):64
S4202 Verapamil HCl Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.
NPJ Precis Oncol, 2024, 8(1):94
Int J Mol Sci, 2024, 25(18)10162
Biomedicines, 2024, 12(4)904
S2187 Avasimibe Avasimibe inhibits ACAT with IC50 of 3.3 μM, also inhibits human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μM, 13.9 μM and 26.5 μM, respectively.
Nat Commun, 2024, 15(1):8301
PLoS Pathog, 2023, 19(5):e1011323
Hepatol Int, 2023, 10.1007/s12072-023-10490-4
S1794 Fenofibrate Fenofibrate is a compound of the fibrate class and fibric acid derivative. Fenofibrate is a selective agonist of PPARα with EC50 of 30 μM. Fenofibrate binds to and inhibits cytochrome P450 epoxygenase (CYP)2C with IC50 of 0.2 μM, 0.7 μM and 9.7 μM for CYP2C19, CYP2B6 and CYP2C9, respectively. Fenofibrate induces autophagy.
Heliyon, 2024, 10(11):e31861
Cancer Lett, 2023, 10.1016/j.canlet.2023.216427
Cell Metab, 2022, 34(2):299-316.e6
S2900 Cobicistat Cobicistat is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S2046 Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.
J Transl Med, 2024, 22(1):593
Commun Biol, 2022, 5(1):231
J Genet Genomics, 2022, S1673-8527(22)00133-3
S2394 Naringenin Naringenin (NSC 34875, S-Dihydrogenistein, NSC 11855, Salipurol) is a natural predominant flavanone derived from plant food, which is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.
J Transl Med, 2024, 22(1):208
J Lipid Res, 2024, S0022-2275(24)00044-0
Molecules, 2023, 28(13)4947
S4662 Atazanavir Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.
Int J Mol Sci, 2022, 23(23)15380
Chemistry, 2022, e202202798.
Sci Rep, 2021, 11(1):19443
S1952 Methoxsalen Methoxsalen (Xanthotoxin, NCI-C55903) is a naturally occurring photoactive substance found in the seeds of the Ammi majus (Umbelliferae) plant, used in the diagnosis and treatment of psoriasis; A CYP2A5/6 inhibitor.
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
S2803 Galeterone Galeterone (TOK-001) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.
ChemMedChem, 2022, e202200043
Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w
Steroids, 2020, 153:108534
S2555 Clarithromycin Clarithromycin (A-56268) is a macrolide antibiotic and a CYP3A4 inhibitor, used to treat a number of bacterial infections.
Microorganisms, 2022, 10(7)1421
Cell Biol Toxicol, 2021, 10.1007/s10565-021-09646-5
J Ovarian Res, 2019, 12(1):107
S5658 Omeprazole Sodium Omeprazole Sodium is the sodium salt form of omeprazole, which is a proton pump inhibitor and suppresses gastric acid secretion. Omeprazole Sodium is a metabolism-dependent inhibitor (MDI) of CYP2C19.
Theranostics, 2021, 11(5):2364-2380
Theranostics, 2021, 11(5):2364-2380
J Virol, 2021, JVI.00190-21
S2380 Diosmetin Diosmetin (Luteolin 4-methyl ether) is a bioflavonoid found in spearmint, oregano, and many other plants.
Mol Med Rep, 2020, 22(2):1335-1341
J Med Virol, 2019, 91(8):1440-1447
Int J Biol Sci, 2019, 15(11):2497-2508
S2526 Alizarin Alizarin is a red coloring mordant dye extracted from the roots of madder plants (Rubia tinctorum L). Alizarin strongly inhibits P450 isoform CYP1A1, CYP1A2, and CYP1B1 with IC50 of 6.2 μM, 10.0 μM, and 2.7 μM, respectively in an enzymatic assay. There are also literature reports Alizarin increases the CYP1A1 enzymatic activity and acts as an agonist to the AHR receptor in HepG2 cells.
Chem Res Toxicol, 2023, 36(8):1361-1373
BMC Med, 2022, 20(1):365
Cell Rep, 2020, 14;31(2):107518
S7456 Osilodrostat (LCI699) LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis.
Cells, 2022, 11(21)3344
Drug Metab Dispos, 2022, 50(2):114-127
J Inorg Biochem, 2022, 235:111934
S1195 Orteronel Orteronel(TAK-700) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). TAK-700 (Orteronel) is an androgen biosynthesis inhibitor. Phase 3.
Toxicol Appl Pharmacol, 2023, 475:116638
Drug Metab Dispos, 2017, 45(6):635-645
Biochem Biophys Res Commun, 2016, 477(4):1005-10
S2401 Sodium Danshensu Sodium Danshensu is a mono sodium of danshensu, which is a natural phenolic acid of caffeic acid derivatives isolated from Salvia miltiorrhiza.
Molecules, 2023, 28(4)1551
Front Pharmacol, 2022, 13:946668
Front Pharmacol, 2022, 13:946668
S3931 Ginsenoside Rd Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Drug Des Devel Ther, 2022, 16:2767-2782
J Ginseng Res, 2022, 46(5):700-709
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S3874 Curcumenol Curcumenol, a sesquiterpene isolated from Curcuma zedoaria, is known to possess a variety of health and medicinal values which includes neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. It inhibits NF-κB activation by suppressing the nuclear translocation of the NF-κB p65 subunit and blocking IκBα phosphorylation and degradation.
Front Pharmacol, 2022, 13:905966
J Bone Miner Res, 2021, 10.1002/jbmr.4328
Int J Mol Med, 2021, 48(4)192
S5266 Stiripentol Stiripentol (BCX2600) is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.
Cell Metab, 2022, 34(1):90-105.e7
Front Pharmacol, 2021, 12:785586
S3673 Sulfaphenazole Sulfaphenazole (Depocid, Depotsulfonamide, Plisulfan, Raziosulfa) is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).
UNIVERSITY OF APPLIED SCIENCES, 2023,
Chem Biol Interact, 2022, 353:109801
Chem Biol Interact, 2022, 365:110070
S3917 Tetrahydrocurcumin Tetrahydrocurcumin (Tetrahydrodiferuloylmethane, Tetrahydro Curcumin), a major metabolite of curcumin, possesses strong antioxidant and cardioprotective properties. Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit CYP2C9 and CYP3A4.
J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
Invest Ophthalmol Vis Sci, 2022, 63(6):26
S3660 Uniconazole (S 3307D) Uniconazole (S 3307D, XE 1019D) is a well known inhibitor of cytochrome P450 monooxygenase that prevents the biosynthesis of trans-zeatin. Uniconazole targets CYP735As with Ki of 22 μM.
Nat Microbiol, 2022, 10.1038/s41564-022-01072-5
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
S2329 Naringin Naringin (Naringoside) is a flavanone glycoside, which exerts a variety of pharmacological effects such as antioxidant activity, blood lipid lowering, anticancer activity, and inhibition of cytochrome P450 enzymes.
Am J Transl Res, 2021, 13(6):6330-6341
Int J Mol Sci, 2020, 21(14):5025
S5416 Metyrapone Metyrapone (NSC-25265, SU-4885) is an inhibitor of the enzyme steroid 11-beta-monooxygenase (CYP11B1) that inhibits adrenal steroid synthesis.
Cells, 2022, 11(21)3344
S3766 Tanshinone IIA sulfonate sodium Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
J Inflamm Res, 2022, 15:6293-6306
S4221 Benzbromarone Benzbromarone(Desuric) is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM.
Hum Mol Genet, 2020, ddaa244
S2344 Piperine Piperine (1-Piperoylpiperidine) is the alkaloid responsible for the pungency of black pepper and long pepper, which has also been used in some forms of traditional medicine and as an insecticide.
Int J Mol Med, 2015, 36(5):1369-76
S2496 Ozagrel Ozagrel (OKY-046) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
S1739 Thiabendazole Thiabendazole inhibits the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property, used as an anthelmintic and fungicide agent. It is a potent inhibitor of cytochrome P450 1A2 (CYP1A2).
S2067 Ozagrel HCl Ozagrel HCl (OKY-046) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
S5169 2,6-Dihydroxyanthraquinone 2,6-Dihydroxyanthraquinone (Anthraflavic acid, Anthraflavin) is a potent and specific inhibitor of cytochrome P-448 activity.
S0721 Ticlopidine Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina,PCR 5332) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP). Ticlopidine is also an inhibitor of CYP2B6 with Ki of 0.2 μM.
S0922 Salvianolic acid C Salvianolic acid C is a non-competitive Cytochrome P4502C8 (CYP2C8) inhibitor and a moderate mixed inhibitor of Cytochrome P45022J2 (CYP2J2).
S2921 PF-4981517 PF-4981517 (CYP3cide, PF-04981517) is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7.
S3273 Hypericin Hypericin (Hyp, HY) is a naturally occurring substance found in the common St. John's Wort (Hypericum species) with antidepressive, antineoplastic and antiviral (human immunodeficiency and hepatitis C virus) activities. Hypericin has inhibitory effects on MAO (monoaminoxidase), PKC (protein kinase C), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450).
Eur J Pharmacol, 2021, 900:174071
S3291 Myristicin Myristicin (Myristicine), a terpene-like active component in Nutmeg which is the seed of Myristica fragrans, is a weak inhibitor of monamine oxidase (MAO) and a mechanism-based inhibitor of CYP1A2.
S5252 Ozagrel sodium Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase (CYP5) inhibitor with neuroprotective properties.
E1650 Opevesostat (ODM208) Opevesostat (ODM208) is the first-in-class, selective, nonsteroidal, oral CYP11A1 inhibitor. ODM208 exhibits a rapid, complete, durable, and reversible inhibition of the steroid hormone biosynthesis in an adrenocortical carcinoma cell model in vitro, in adult noncastrated male mice and dogs, and in patients with CRPC.
S0541 Dazoxiben hydrochloride Dazoxiben hydrochloride (HCl) is a potent, selevtive and orally active inhibitor of thromboxane (TX) synthase. Dazoxiben inhibits TXB2 production in clotting human whole blood with IC50 of 0.3 μM and causes parallel enhancement of PGE2 production.
S9250 Isosilybin Isosilybin (Silymarin, Isosilybinin, Q-100795) is a flavanolignan found in the extract of S. marianum fruits with antioxidant and anticancer activities. Isosilybin inhibits CYP3A4 induction with an IC50 of 74 μM.
S9257 Acetylshikonin Acetylshikonin is a biologically active compound with anti-cancer and anti-inflammatory activity, which is isolated from the roots of Lithospermum erythrorhizoma. It is a novel general P450 inhibitor with IC50 values of 1.4-4.0 μM for all tested P450s.
E0214 Pachymic acid Pachymic acid(3-O-Acetyltumulosic acid) inhibits the activity of CYP2C9 with the IC50 of 21.25 µM.
S4938 Cedrol Cedrol, a natural occuring sesquiterpene alcohol, is a potent competitive inhibitor of CYP2B6-mediated bupropion hydroxylase with inhibition constant (Ki) value of 0.9 μM. It also inhibits CYP3A4-mediated midazolam hydroxylation with a Ki value of 3.4 μM while only weakly inhibits CYP2C8, CYP2C9, and CYP2C19 activities.
S2389 Naringin Dihydrochalcone Naringin Dihydrochalcone(Naringin DC) is a new-style sweetening agent and an artificial sweetener derived from naringin and also an inhibitor of CYP enzymes.
E4855New Sertaconazole Sertaconazole(FI-7045) is an imidazole-type antifungal agent that inhibits ergosterol biosynthesis by inhibiting the cytochrome P450-dependent 14α-lanosterol demethylase or Erg11p. This inhibition disrupts fungal cell membrane integrity, ultimately leading to fungal cell death. Sertaconazole is used in the topical treatment of superficial mycoses.
S9299 Ginsenoside F1 Ginsenoside F1, a pharmaceutical component of ginseng, is known to have antiaging, antioxidant, anticancer, and keratinocyte protective effects. Ginsenoside F1 exhibits competitive inhibition of the activity of CYP3A4 with Ki values of 67.8 ± 16.2 μM. Ginsenoside F1 also exhibited a weaker inhibition of the activity of CYP2D6.
S4963 Purpurin Purpurin (1,2,4-Trihydroxyanthraquinone, Hydroxylizaric acid, Verantin) is one of the natural colorants extracted from madder roots and other Rubiaceae family plants. It exhibits anti-angiogenic, antifungal, antibiotic, and antioxidative activities. Purpurin strongly inhibits the activities of CYP1A1, CYP1A2 and CYP1B1.
E0531 TMS TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive human cytochrome P450s B1 (CYP1B1) inhibitor with an IC50 of 6 nM.
S3777 Gentiopicroside Gentiopicroside (GE, Gentiopicrin), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.
S0110 APD597 APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
S4831 Piperonyl butoxide Piperonyl butoxide (PBO, Butacide, Ethanol butoxide, Pyrenone 606,ENT-14250) is a man-made pesticide synergist, working with insect killers to increase their effectiveness.Piperonyl butoxide is an inhibitor of cytochrome P450 monooxygenases(P450s).
E1830New Baxdrostat Baxdrostat(CIN-107) is a selective and potent inhibitor of aldosterone synthase(CYP11B2), a rate-limiting enzyme in the pathway of aldosterone synthesis, with the potential to treat resistant hypertension. It also inhibits the function of multidrug and toxin extrusion 1 (MATE1) and MATE2-K with IC50 values of 1.34 µM and 2.67 µM, respectively.
E2912 MEHP MEHP (Phthalic acid mono-2-ethylexyl ester) is a competitive inhibitor of CYP2C9 with IC50 of 6.37 μM.
S0175 DMU2105 DMU2105 is a potent and specific inhibitor of CYP1B1 with IC50 of 10 nM.
S0176 DMU2139 DMU2139 is a potent and specific inhibitor of CYP1B1 with IC50 of 9 nM.
S0418 Ezutromid Ezutromid (SMT C1100,BMN 195,VOX-C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM which can be used for the research Duchenne muscular dystrophy (DMD), also inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM.
S3719 Topiroxostat Topiroxostat is a xanthine oxidoreductase (XOR) inhibitor and used for treatment of gout and hyperuricemia. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment.
S2571New Quinidine Quinidine is a pharmaceutical agent that acts as a class I antiarrhythmic agent.
S6886 1-Aminobenzotriazole 1-Aminobenzotriazole (ABT, 3-Aminobenzotriazole, 1-Benzotriazolylamine, NSC 114498, NSC 656987) is a nonselective and irreversible inhibitor of cytochrome P450 (CYP) enzymes. 1-Aminobenzotriazole is also a substrate and inhibitor of N-acetyltransferase (NAT).
S9442 Bergaptol Bergaptol (5-Hydroxypsoralen, 5-Hydroxyfuranocoumarin) is a natural furanocoumarin found in the essential oils of citrus including lemon and bergamot.Bergaptol is a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 μM.
Molecules, 2024, 29(3)713
S5380 7-Hydroxyflavone 7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines.
S5529 Galangin Galangin (3,5,7-trihydroxyflavone; Norizalpinin), a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.
S9241 Polygalaxanthone III Polygalaxanthone III is a natural product with the efficacy of tranquilization, glaangal, eliminating sputum and detumescence. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.
S6594 Liarozole dihydrochloride Liarozole Dihydrochloride is identified as a modest inhibitor of P450 with IC50 of 2.2–6.0 μM and 260 nM for CYP26 and rat CYP17 respectively.
S9163 Rhapontigenin Rhapontigenin (Protigenin), produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM).
S0230 NVP-VID-400 NVP-VID-400 (SDZ285428) is an inhibitor of CYP51. NVP-VID-400 (SDZ285428) inhibits T. cruzi and T. brucei with I/E2a(5 min) of both <1 and I/E2(60 min) of 9 and 35, respectively.
S3227 5,7-Dimethoxyflavone 5,7-Dimethoxyflavone (5,7-DMF) is an inhibitor of cytochrome P450 (CYP) 3As that markedly decreases the expression of CYP3A11 and CYP3A25 in the liver. 5,7-Dimethoxyflavone (5,7-DMF) is also a potent Breast Cancer Resistance Protein (BCRP, ABCG2) inhibitor. 5,7-Dimethoxyflavone (5,7-DMF) is one of the major components of Kaempferia parviflora with anti-obesity, anti-inflammatory, and antineoplastic effects.
S6437 Oxolamine Citrate Oxolamine (SKF-9976, AF-438) citrate, a cough suppressant, is an inhibitor of CYP2B1/2. Oxolamine citrate also exhibits anti-inflammatory effect.
S6868 Alflutinib (Furmonertinib) mesylate Alflutinib (Furmonertinib) mesylate is a third-generation epidermal growth factor receptor (EGFR) inhibitor that inhibits both EGFR-sensitive mutations and T790M mutations. Alflutinib (AST2818), primarily metabolized by CYP3A4, is also a potent CYP3A4 inducer with EC50 of 0.25 μM.
Biomedicines, 2024, 12(7)1412
Int J Mol Sci, 2023, 24(18)13972
Int J Mol Sci, 2023, 24(18)13972
S5967 Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Front Biosci (Landmark Ed), 2022, 27(8):242
Front Pharmacol, 2021, 12:632201
S2271 Berberine chloride Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Adv Healthc Mater, 2023, e2300591.
Transl Oncol, 2023, 35:101712
J Biomol Struct Dyn, 2022, 1-11
S4784 Phloracetophenone Phloracetophenone, or 2,4,6-trihydroxyacetophenone (THA), the aglycone component of phloracetophenone glucoside, is a naturally occurring compound obtained from the rhizome of Curcuma comosa (Family Zingiberaceae). Phloracetophenone can stimulate CYP7A1 activity. Phloracetophenone induces cholestasis in rats mediated through Mrp2.
S6606 CDD3505 CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
S5969 Dicloxacillin Sodium hydrate Dicloxacillin Sodium hydrate (DLX, Dycill, Dynapen, Pathocil), a narrow-spectrum β-Lactam antibiotic of the penicillin class, induces drug-metabolizing CYP enzymes to a clinically relevant extent.
E4855New Sertaconazole Sertaconazole(FI-7045) is an imidazole-type antifungal agent that inhibits ergosterol biosynthesis by inhibiting the cytochrome P450-dependent 14α-lanosterol demethylase or Erg11p. This inhibition disrupts fungal cell membrane integrity, ultimately leading to fungal cell death. Sertaconazole is used in the topical treatment of superficial mycoses.
E1830New Baxdrostat Baxdrostat(CIN-107) is a selective and potent inhibitor of aldosterone synthase(CYP11B2), a rate-limiting enzyme in the pathway of aldosterone synthesis, with the potential to treat resistant hypertension. It also inhibits the function of multidrug and toxin extrusion 1 (MATE1) and MATE2-K with IC50 values of 1.34 µM and 2.67 µM, respectively.
S2571New Quinidine Quinidine is a pharmaceutical agent that acts as a class I antiarrhythmic agent.

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