Histone Acetyltransferase

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

Histone Acetyltransferase Products

All (19) Histone Acetyltransferase Inhibitors (18) Histone Acetyltransferase Activators (1)

Catalog No.	Information	Product Use Citations	Product Validations
S7152	C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a K_i of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.	Cancer Lett, 2021, 513:36-49 Sci Rep, 2021, 11(1):10078 Cell Cycle, 2021, 20(4):392-405	Phosphorylation of STAT6 in butyrate-treated M2-BMDMs. Western blotting was performed with anti-phospho-STAT6, STAT6, and β-actin. Data are representative of three independent experiments. M2:M2 macrophage; But:butyrate.
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.	Front Immunol, 2021, 12:656242 Aging (Albany NY), 2021, 13(10):13968-14000 Biomolecules, 2021, 11(5)674
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.	Immunity, 2021, S1074-7613(21)00222-3 Clin Cancer Res, 2021, clincanres.4391.2020 Clin Sci (Lond), 2021, 135(3):555-574	H3K27ac change. SMMC-7721 cells were treated with EPZ-6438 (1 μM) alone or in combination with histone acetyltransferase inhibitors C646 (5 μM) or SGC-CBP30 (5 μM) for 6 days. H3K27ac was examined by immunoblotting.
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.	Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0237-5
S9805^New	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.
S1161^New	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.
S1242^New	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.
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.	Mol Cell, 2021, S1097-2765(21)00051-4 Cell Death Dis, 2021, 12(5):419 Int J Radiat Oncol Biol Phys, 2021, 110(4):1210-1221
S6655	WM-8014 WM-8014 is a highly potent inhibitor of histone acetyltransferase KAT6A with an IC50 of 8 nM.
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.	Theranostics, 2021, 11(13):6278-6292 Theriogenology, 2021, 159:140-146 J Med Chem, 2020, 31
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.	Oncogene, 2020, 39(18):3754-3773 Free Radic Biol Med, 2020, 10.1016/j.freeradbiomed.2020.01.016 Chemosphere, 2020, 247:125825	Western blot analysis of α-SMA expression in whole-lung lysates. Data are expressed as means ± SEM, *P < 0.05 versus vehicle and #P < 0.05 versus PQ (n = 4-6).
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.
S7641	Remodelin hydrobromide Remodelin hydrobromide (HBr) is a potent acetyl-transferase NAT10 inhibitor.	Transl Oncol, 2020, 16;13(8):100783 Mol Cell Biochem, 2020, 10.1007/s11010-020-03776-w Cell Rep, 2019, 29(7):2078-2091.e5
S2951	P300/CBP-IN-3 P300/CBP-IN-3 is an inhibitor of p300/CBP histone acetyltransferase.
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).	Neurochem Res, 2021, 10.1007/s11064-021-03260-x
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).
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.	Biomolecules, 2021, 11(5)658 bioRxiv, 2021, 2021.04.21.440833 J Clin Invest, 2020, 2;130(3):1431-1445
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.

Catalog No.	Information	Product Use Citations	Product Validations
S7152	C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a K_i of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.	Cancer Lett, 2021, 513:36-49 Sci Rep, 2021, 11(1):10078 Cell Cycle, 2021, 20(4):392-405	Phosphorylation of STAT6 in butyrate-treated M2-BMDMs. Western blotting was performed with anti-phospho-STAT6, STAT6, and β-actin. Data are representative of three independent experiments. M2:M2 macrophage; But:butyrate.
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.	Front Immunol, 2021, 12:656242 Aging (Albany NY), 2021, 13(10):13968-14000 Biomolecules, 2021, 11(5)674
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.	Immunity, 2021, S1074-7613(21)00222-3 Clin Cancer Res, 2021, clincanres.4391.2020 Clin Sci (Lond), 2021, 135(3):555-574	H3K27ac change. SMMC-7721 cells were treated with EPZ-6438 (1 μM) alone or in combination with histone acetyltransferase inhibitors C646 (5 μM) or SGC-CBP30 (5 μM) for 6 days. H3K27ac was examined by immunoblotting.
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.	Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0237-5
S9805^New	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.
S1161^New	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.
S1242^New	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.
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.	Mol Cell, 2021, S1097-2765(21)00051-4 Cell Death Dis, 2021, 12(5):419 Int J Radiat Oncol Biol Phys, 2021, 110(4):1210-1221
S6655	WM-8014 WM-8014 is a highly potent inhibitor of histone acetyltransferase KAT6A with an IC50 of 8 nM.
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.	Theranostics, 2021, 11(13):6278-6292 Theriogenology, 2021, 159:140-146 J Med Chem, 2020, 31
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.	Oncogene, 2020, 39(18):3754-3773 Free Radic Biol Med, 2020, 10.1016/j.freeradbiomed.2020.01.016 Chemosphere, 2020, 247:125825	Western blot analysis of α-SMA expression in whole-lung lysates. Data are expressed as means ± SEM, *P < 0.05 versus vehicle and #P < 0.05 versus PQ (n = 4-6).
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.
S7641	Remodelin hydrobromide Remodelin hydrobromide (HBr) is a potent acetyl-transferase NAT10 inhibitor.	Transl Oncol, 2020, 16;13(8):100783 Mol Cell Biochem, 2020, 10.1007/s11010-020-03776-w Cell Rep, 2019, 29(7):2078-2091.e5
S2951	P300/CBP-IN-3 P300/CBP-IN-3 is an inhibitor of p300/CBP histone acetyltransferase.
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).	Neurochem Res, 2021, 10.1007/s11064-021-03260-x
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).
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.	Biomolecules, 2021, 11(5)658 bioRxiv, 2021, 2021.04.21.440833 J Clin Invest, 2020, 2;130(3):1431-1445

Catalog No.	Information	Product Use Citations	Product Validations
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.

Catalog No.

Information

Product Use Citations

Product Validations

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.