S7152 |
C646
|
C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy. |
-
Nat Commun, 2024, 15(1):5209
-
Cell Commun Signal, 2024, 22(1):117
-
Antioxidants (Basel), 2024, 13(4)424
|
|
S1848 |
Curcumin
|
Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on. |
-
Cancer Cell Int, 2024, 24(1):303
-
Front Pharmacol, 2024, 15:1418902
-
PLoS Negl Trop Dis, 2024, 18(8):e0012428
|
|
S7256 |
SGC-CBP30
|
SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively. |
-
Cell Rep, 2023, 42(8):112963
-
Cell Rep, 2023, 42(6):112547
-
J Hepatol, 2022, 76(4):921-933
|
|
S7582 |
Anacardic Acid
|
Anacardic Acid (6-pentadecylsalicylic Acid) is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases, which also has antibacterial activity, antimicrobial activity,
prostaglandin synthase inhibition, and tyrosinase and lipoxygenase inhibition.
|
-
POLYU ELECTRONIC THESES, 2023, viii, 164
-
Hepatology, 2021, 10.1002/hep.32245
-
Hepatology, 2021, 10.1002/hep.32245
|
|
S7476 |
MG149
|
MG149 (Tip60 HAT inhibitor) is a potent histone acetyltransferase inhibitor with IC50 of 74 μM and 47 μM for Tip60 and MOF,respectively.
|
-
Clin Exp Hypertens, 2023, 45(1):2259130
-
iScience, 2023, 26(12):108446
-
Int J Mol Sci, 2023, 24(10)8719
|
|
S8740 |
A-485
|
A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets. |
-
Cell Rep, 2024, 43(8):114529
-
Ecotoxicol Environ Saf, 2024, 270:115877
-
Cancers (Basel), 2024, 16(9)1622
|
|
S7641 |
Remodelin hydrobromide
|
Remodelin hydrobromide (HBr) is a potent acetyl-transferase NAT10 inhibitor.
|
-
Nat Commun, 2024, 15(1):2137
-
Redox Biol, 2024, 72:103145
-
J Adv Res, 2024, S2090-1232(24)00318-7
|
|
S8776 |
WM-1119
|
WM-1119 is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with IC50 of 0.25 μM. It is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively. |
-
Cancer Discov, 2022, candisc.0646.2021
-
Theranostics, 2021, 11(13):6278-6292
-
Biochem Biophys Res Commun, 2021, 585:185-190
|
|
S9648 |
NEO2734
|
NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM. |
-
Cell Rep Med, 2024, 5(3):101471
-
Nat Cancer, 2023, 4(10):1508-1525
-
PLoS Pathog, 2023, 19(8):e1011598
|
|
S8190 |
CPI-637
|
CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9. |
-
Mol Cell Proteomics, 2023, 22(3):100504
-
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0237-5
|
|
S9432 |
Ginkgolic Acid
|
Ginkgolic acid, toxic phenolic compounds present in the fruits and leaves of Ginkgo biloba L., is a potent sumoylation inhibitor also reported to inhibit histone acetylation transferase (HAT). |
-
Pharmaceutics, 2024, 16(5)638
-
CNS Neurosci Ther, 2022, 10.1111/cns.13871
-
Neurochem Res, 2021, 10.1007/s11064-021-03260-x
|
|
S0022 |
YF-2
|
YF-2 is a highly selective, blood-brain-barrier permeable activator of histone acetyltransferase (HAT). In In vitro assays, YF-2 has activity versus CBP, PCAF, and GCN5 with EC50 of 2.75 μΜ, 29.04 μΜ and 49.3 μΜ, respectively. YF-2 also increases p300 activity. |
-
J Exp Clin Cancer Res, 2022, 41(1):77
|
|
S1242 |
CPTH2
|
CPTH2 is a potent histone acetyltransferase (HAT) inhibitor modulating Gcn5p network. CPTH2 induces apoptosis and decreases the invasiveness of a ccRCC cell line through the inhibition of KAT3B. |
-
Transl Oncol, 2021, 14(11):101196
|
|
S1161 |
Histone Acetyltransferase Inhibitor II
|
Histone Acetyltransferase Inhibitor II (HAT Inhibitor II, compound 2c) is a potent, selective and cell-permeable p300 histone acetyltransferase (HAT) inhibitor with IC50 of 5 μM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.
|
-
Genetics, 2017, 205(3):1125-1137
|
|
E1107 |
CTB
|
CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol. |
|
|
S7475New |
NU9056
|
NU9056 is a potent and selective inhibitor of Tip60 (KAT5) histone acetyltransferase with an IC50 value of 2 µM. NU9056 demonstrates over 16-fold selectivity for Tip60 compared to PCAF, p300, and GCN5 and effectively induces apoptosis in prostate cancer cells. |
|
|
S6655 |
WM-8014
|
WM-8014 is a highly potent inhibitor of histone acetyltransferase KAT6A with an IC50 of 8 nM. |
|
|
E1215 |
JQAD1
|
JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. |
-
bioRxiv, 2024, 2024.03.29.587346
|
|
E0068 |
NiCur
|
NiCur is a small molecule which blocks CREB-binding protein (CBP) histone acetyltransferase (HAT) activity and downregulates p53 activation upon genotoxic stress and diminishs the recruitment of p53 as well as RNA Polymerase II and levels of acetylation on histone H3 on CDKN1A promoter. |
|
|
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). |
|
|
S9445 |
Ginkgolic Acid (C13:0)
|
Ginkgolic Acid (C13:0) is a natural anticariogenic agent in Ginkgo biloba L. that exhibits antimicrobial activity against S. mutans and suppresses the specific virulence factors associated with its cariogenicity. Ginkgolic acid is a potent sumoylation inhibitor and reported to inhibit histone acetylation transferase (HAT). |
|
|
S2977 |
EML 425
|
EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively. |
-
bioRxiv, 2024, 2024.02.22.581432
|
|
S9805 |
WM-3835
|
WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation. |
|
|
E0146 |
PF-9363
|
PF-9363 is a potent and selective KAT6A/6B inhibitor with Ki of 0.41 nM and 1.2 nM for KAT6A and KAT6B, respectively. PF-9363 displays potent anti-tumor activity in ER+ breast cancer models.
|
|
|
S7152 |
C646
|
C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy. |
- Nat Commun, 2024, 15(1):5209
- Cell Commun Signal, 2024, 22(1):117
- Antioxidants (Basel), 2024, 13(4)424
|
|
S1848 |
Curcumin
|
Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on. |
- Cancer Cell Int, 2024, 24(1):303
- Front Pharmacol, 2024, 15:1418902
- PLoS Negl Trop Dis, 2024, 18(8):e0012428
|
|
S7256 |
SGC-CBP30
|
SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. Exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively. |
- Cell Rep, 2023, 42(8):112963
- Cell Rep, 2023, 42(6):112547
- J Hepatol, 2022, 76(4):921-933
|
|
S7582 |
Anacardic Acid
|
Anacardic Acid (6-pentadecylsalicylic Acid) is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases, which also has antibacterial activity, antimicrobial activity,
prostaglandin synthase inhibition, and tyrosinase and lipoxygenase inhibition.
|
- POLYU ELECTRONIC THESES, 2023, viii, 164
- Hepatology, 2021, 10.1002/hep.32245
- Hepatology, 2021, 10.1002/hep.32245
|
|
S7476 |
MG149
|
MG149 (Tip60 HAT inhibitor) is a potent histone acetyltransferase inhibitor with IC50 of 74 μM and 47 μM for Tip60 and MOF,respectively.
|
- Clin Exp Hypertens, 2023, 45(1):2259130
- iScience, 2023, 26(12):108446
- Int J Mol Sci, 2023, 24(10)8719
|
|
S8740 |
A-485
|
A-485 is a potent, selective and drug-like p300/CBP catalytic inhibitor with an IC50 of 0.06 μM for p300 HAT. It is selective over BET bromodomain proteins and >150 non-epigenetic targets. |
- Cell Rep, 2024, 43(8):114529
- Ecotoxicol Environ Saf, 2024, 270:115877
- Cancers (Basel), 2024, 16(9)1622
|
|
S7641 |
Remodelin hydrobromide
|
Remodelin hydrobromide (HBr) is a potent acetyl-transferase NAT10 inhibitor.
|
- Nat Commun, 2024, 15(1):2137
- Redox Biol, 2024, 72:103145
- J Adv Res, 2024, S2090-1232(24)00318-7
|
|
S8776 |
WM-1119
|
WM-1119 is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with IC50 of 0.25 μM. It is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively. |
- Cancer Discov, 2022, candisc.0646.2021
- Theranostics, 2021, 11(13):6278-6292
- Biochem Biophys Res Commun, 2021, 585:185-190
|
|
S9648 |
NEO2734
|
NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM. |
- Cell Rep Med, 2024, 5(3):101471
- Nat Cancer, 2023, 4(10):1508-1525
- PLoS Pathog, 2023, 19(8):e1011598
|
|
S8190 |
CPI-637
|
CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9. |
- Mol Cell Proteomics, 2023, 22(3):100504
- Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0237-5
|
|
S9432 |
Ginkgolic Acid
|
Ginkgolic acid, toxic phenolic compounds present in the fruits and leaves of Ginkgo biloba L., is a potent sumoylation inhibitor also reported to inhibit histone acetylation transferase (HAT). |
- Pharmaceutics, 2024, 16(5)638
- CNS Neurosci Ther, 2022, 10.1111/cns.13871
- Neurochem Res, 2021, 10.1007/s11064-021-03260-x
|
|
S1242 |
CPTH2
|
CPTH2 is a potent histone acetyltransferase (HAT) inhibitor modulating Gcn5p network. CPTH2 induces apoptosis and decreases the invasiveness of a ccRCC cell line through the inhibition of KAT3B. |
- Transl Oncol, 2021, 14(11):101196
|
|
S1161 |
Histone Acetyltransferase Inhibitor II
|
Histone Acetyltransferase Inhibitor II (HAT Inhibitor II, compound 2c) is a potent, selective and cell-permeable p300 histone acetyltransferase (HAT) inhibitor with IC50 of 5 μM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.
|
- Genetics, 2017, 205(3):1125-1137
|
|
S7475New |
NU9056
|
NU9056 is a potent and selective inhibitor of Tip60 (KAT5) histone acetyltransferase with an IC50 value of 2 µM. NU9056 demonstrates over 16-fold selectivity for Tip60 compared to PCAF, p300, and GCN5 and effectively induces apoptosis in prostate cancer cells. |
|
|
S6655 |
WM-8014
|
WM-8014 is a highly potent inhibitor of histone acetyltransferase KAT6A with an IC50 of 8 nM. |
|
|
E0068 |
NiCur
|
NiCur is a small molecule which blocks CREB-binding protein (CBP) histone acetyltransferase (HAT) activity and downregulates p53 activation upon genotoxic stress and diminishs the recruitment of p53 as well as RNA Polymerase II and levels of acetylation on histone H3 on CDKN1A promoter. |
|
|
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). |
|
|
S9445 |
Ginkgolic Acid (C13:0)
|
Ginkgolic Acid (C13:0) is a natural anticariogenic agent in Ginkgo biloba L. that exhibits antimicrobial activity against S. mutans and suppresses the specific virulence factors associated with its cariogenicity. Ginkgolic acid is a potent sumoylation inhibitor and reported to inhibit histone acetylation transferase (HAT). |
|
|
S2977 |
EML 425
|
EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively. |
- bioRxiv, 2024, 2024.02.22.581432
|
|
S9805 |
WM-3835
|
WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation. |
|
|
E0146 |
PF-9363
|
PF-9363 is a potent and selective KAT6A/6B inhibitor with Ki of 0.41 nM and 1.2 nM for KAT6A and KAT6B, respectively. PF-9363 displays potent anti-tumor activity in ER+ breast cancer models.
|
|
|