Histone Acetyltransferase

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Histone Acetyltransferase製品

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  • Histone Acetyltransferase阻害剤 (20)
  • Histone Acetyltransferase活性剤(3)
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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.
Cell Commun Signal, 2024, 22(1):117
Mol Carcinog, 2024, 63(3):430-447
Research Square, 2024, 10.21203/rs.3.rs-3834927/v1
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.
Nutrients, 2023, 15(3)740
Phytother Res, 2022, 36(3):1326-1337
Oncol Rep, 2022, 48(6)221
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
Int J Mol Sci, 2023, 24(10)8719
Brain Behav Immun, 2022, S0889-1591(22)00025-3
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.
bioRxiv, 2024, 2024.02.02.578660
Nat Commun, 2023, 14(1):8361
Gut Microbes, 2023, 15(2):2249143
S7641 Remodelin hydrobromide Remodelin hydrobromide (HBr) is a potent acetyl-transferase NAT10 inhibitor.
Mol Med, 2024, 30(1):13
Adv Sci (Weinh), 2023, 10(23):e2300898
J Exp Clin Cancer Res, 2023, 42(1):9
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.
Nat Cancer, 2023, 4(10):1508-1525
Nat Cancer, 2023, 10.1038/s43018-023-00635-7
Br J Cancer, 2022, 10.1038/s41416-022-01815-5
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).
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.
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.
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.
E1654New 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.
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.
Cell Commun Signal, 2024, 22(1):117
Mol Carcinog, 2024, 63(3):430-447
Research Square, 2024, 10.21203/rs.3.rs-3834927/v1
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.
Nutrients, 2023, 15(3)740
Phytother Res, 2022, 36(3):1326-1337
Oncol Rep, 2022, 48(6)221
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
Int J Mol Sci, 2023, 24(10)8719
Brain Behav Immun, 2022, S0889-1591(22)00025-3
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.
bioRxiv, 2024, 2024.02.02.578660
Nat Commun, 2023, 14(1):8361
Gut Microbes, 2023, 15(2):2249143
S7641 Remodelin hydrobromide Remodelin hydrobromide (HBr) is a potent acetyl-transferase NAT10 inhibitor.
Mol Med, 2024, 30(1):13
Adv Sci (Weinh), 2023, 10(23):e2300898
J Exp Clin Cancer Res, 2023, 42(1):9
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.
Nat Cancer, 2023, 4(10):1508-1525
Nat Cancer, 2023, 10.1038/s43018-023-00635-7
Br J Cancer, 2022, 10.1038/s41416-022-01815-5
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).
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
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.
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.
E1654New 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.
E1654New 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.

Histone Acetyltransferase阻害剤の選択性比較

Tags: Histone Acetyltransferase inhibitor|Histone Acetyltransferase agonist|Histone Acetyltransferase activator|Histone Acetyltransferase inducer|Histone Acetyltransferase antagonist|Histone Acetyltransferase signaling pathway|Histone Acetyltransferase assay kit