Histone Acetyltransferase

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Histone Acetyltransferase Signaling Pathway Map

Histone Acetyltransferase Signaling Pathways

Histone Acetyltransferase Products

  • All (21)
  • Histone Acetyltransferase Inhibitors (19)
  • Histone Acetyltransferase Activators (2)
  • New Histone Acetyltransferase Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0146New PF-9363 (CTx-648)

PF-9363 (CTx-648) 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.

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.

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
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.
Phytother Res, 2022, 36(3):1326-1337
Dis Markers, 2022, 2022:3129781
Adv Sci (Weinh), 2021, e2103360
S2951 P300/​CBP-IN-3 P300/CBP-IN-3 is an inhibitor of p300/CBP histone acetyltransferase.
S6655 WM-8014 WM-8014 is a highly potent inhibitor of histone acetyltransferase KAT6A with an IC50 of 8 nM.
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).
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 Rep, 2022, 38(3):110250
Biochim Biophys Acta Gene Regul Mech, 2022, 1865(6):194829
Hepatology, 2021, 10.1002/hep.32245
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.
Nature, 2021, 10.1038/s41586-021-04116-8
Immunity, 2021, S1074-7613(21)00222-3
Sci Adv, 2021, 7(36):eabf9975
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.
Brain Behav Immun, 2022, S0889-1591(22)00025-3
Brain Res Bull, 2022, 184:24-33
Biomolecules, 2021, 11(5)658
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.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
J Pharmacol Exp Ther, 2021, 379(3):303-309
S7641 Remodelin hydrobromide Remodelin hydrobromide (HBr) is a potent acetyl-transferase NAT10 inhibitor.
Cancer Cell Int, 2021, 21(1):413
Transl Oncol, 2020, 16;13(8):100783
Mol Cell Biochem, 2020, 10.1007/s11010-020-03776-w
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
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.
Nat Cell Biol, 2022, 24(3):384-399
EMBO J, 2022, e109463
Br J Cancer, 2022, 10.1038/s41416-022-01815-5
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
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
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).
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.
Br J Cancer, 2022, 10.1038/s41416-022-01815-5
S9805New 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.
E1107New CTB CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol.
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
E0146New PF-9363 (CTx-648)

PF-9363 (CTx-648) 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.

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.

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
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.
Phytother Res, 2022, 36(3):1326-1337
Dis Markers, 2022, 2022:3129781
Adv Sci (Weinh), 2021, e2103360
S2951 P300/​CBP-IN-3 P300/CBP-IN-3 is an inhibitor of p300/CBP histone acetyltransferase.
S6655 WM-8014 WM-8014 is a highly potent inhibitor of histone acetyltransferase KAT6A with an IC50 of 8 nM.
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).
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 Rep, 2022, 38(3):110250
Biochim Biophys Acta Gene Regul Mech, 2022, 1865(6):194829
Hepatology, 2021, 10.1002/hep.32245
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.
Nature, 2021, 10.1038/s41586-021-04116-8
Immunity, 2021, S1074-7613(21)00222-3
Sci Adv, 2021, 7(36):eabf9975
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.
Brain Behav Immun, 2022, S0889-1591(22)00025-3
Brain Res Bull, 2022, 184:24-33
Biomolecules, 2021, 11(5)658
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.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
J Pharmacol Exp Ther, 2021, 379(3):303-309
S7641 Remodelin hydrobromide Remodelin hydrobromide (HBr) is a potent acetyl-transferase NAT10 inhibitor.
Cancer Cell Int, 2021, 21(1):413
Transl Oncol, 2020, 16;13(8):100783
Mol Cell Biochem, 2020, 10.1007/s11010-020-03776-w
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
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.
Nat Cell Biol, 2022, 24(3):384-399
EMBO J, 2022, e109463
Br J Cancer, 2022, 10.1038/s41416-022-01815-5
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
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
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).
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.
Br J Cancer, 2022, 10.1038/s41416-022-01815-5
S9805New 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.
E1107New CTB CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol.
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
E0146New PF-9363 (CTx-648)

PF-9363 (CTx-648) 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.

S9805New 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.
E1107New CTB CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol.
Tags: Histone Acetyltransferase inhibitor|Histone Acetyltransferase agonist|Histone Acetyltransferase activator|Histone Acetyltransferase inducer|Histone Acetyltransferase antagonist|Histone Acetyltransferase signaling pathway|Histone Acetyltransferase assay kit