Histone Acetyltransferase

亜型選択性的な製品

HAT MYST GNAT p300/CBP

シグナル伝達経路

Histone Acetyltransferase製品

All (25)
Histone Acetyltransferase阻害剤 (21)
Histone Acetyltransferase活性剤(3)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
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.	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 Syst, 2023, 14(6):482-500.e8 Cell Rep, 2023, 42(8):112963 Cell Rep, 2023, 42(6):112547
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.	Int J Mol Sci, 2024, 25(17)9600 POLYU ELECTRONIC THESES, 2023, viii, 164 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.	Int J Mol Sci, 2024, 25(17)9600 Clin Exp Hypertens, 2023, 45(1):2259130 iScience, 2023, 26(12):108446
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 Cell Biol, 2024, Nat Commun, 2024, 15(1):2137 Redox Biol, 2024, 72:103145
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.	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.
S7475^New	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.
E1654	CTPB	CTPB is a synthetic activator of the p300 histone acetyltransferase (HAT) enzyme, which promotes transcription by increasing the H3 and H4 acetylation in nucleosomes.
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 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.	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 Syst, 2023, 14(6):482-500.e8 Cell Rep, 2023, 42(8):112963 Cell Rep, 2023, 42(6):112547
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.	Int J Mol Sci, 2024, 25(17)9600 POLYU ELECTRONIC THESES, 2023, viii, 164 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.	Int J Mol Sci, 2024, 25(17)9600 Clin Exp Hypertens, 2023, 45(1):2259130 iScience, 2023, 26(12):108446
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 Cell Biol, 2024, Nat Commun, 2024, 15(1):2137 Redox Biol, 2024, 72:103145
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.	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
S7475^New	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.
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
E1107	CTB	CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol.
E1654	CTPB	CTPB is a synthetic activator of the p300 histone acetyltransferase (HAT) enzyme, which promotes transcription by increasing the H3 and H4 acetylation in nucleosomes.
S7475^New	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.

Histone Acetyltransferase阻害剤の選択性比較