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Histone Acetyltransferase

Histone acetyltransferases (HATs) are enzymes that acetylate conserved lysine amino acids on histone proteins by transferring an acetyl group from acetyl-CoA to form ε-N-acetyllysine. DNA is wrapped around histones, and, by transferring an acetyl group to the histones, genes can be turned on and off. In general, histone acetylation increases gene expression.

A-485
T140731889279-16-6
A-485 is a potent and selective catalytic p300/CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP.
  • $85
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Curcumin
Turmeric yellow, Natural Yellow 3, Indian Saffron, Diferuloylmethane
T1516458-37-7
Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.
  • $37
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NEO2734
EP31670
T86582081072-29-7In house
NEO2734 (EP31670) is an orally active, selective inhibitor of p300/CBP and BET bromodomains, with an IC50 of less than 30 nM for both targets.
  • $116
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WM-3835
T91022229025-70-9
WM-3835 is a novel and high-specific small molecule inhibitor of Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) , able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation.
  • $31
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C646
T2452328968-36-1
C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).
  • $41
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Pocenbrodib
P-300, FT-7051
T696912304372-79-8In house
Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.
  • $790
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Acetaminophen
Paracetamol, APAP, 4'-Hydroxyacetanilide, 4-Acetamidophenol
T0065103-90-2
Acetaminophen (APAP) is a COX inhibitor that inhibits COX-1 and COX-2 (IC50=113.7/25.8 μM). Acetaminophen has antipyretic and analgesic activity as well as weak anti-inflammatory activity.
  • $50
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Remodelin
T3499949912-58-7
Remodelin is an effective and specific inhibitor of the acetyl-transferase protein NAT10.
  • $33
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GNE-781
T154051936422-33-1
GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).
  • $140
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WM-1119
WM1119
T46792055397-28-7
WM-1119 is a highly potent, selective KAT6A/B inhibitor
  • $47
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Butyrolactone 3
MB-3, MB3, MB 3
T14839778649-18-6
Butyrolactone 3 (MB-3) is a histone acetyltransferase Gcn5 inhibitor with a weak affinity for CBP.Butyrolactone 3 has antimicrobial activity and has been used in cancer, metabolic and neurological disorders.
  • $67
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MG 149
Tip60 HAT inhibitor, MG149
T65841243583-85-8
MG 149 (Tip60 HAT inhibitor) is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF(IC50= 47 uM).
  • $48
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PF-9363
CTX-3648
T91672569009-58-9
PF-9363 (CTX-3648) is a potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer.
  • $67
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Anacardic Acid
Hydroginkgolic acid, 6-pentadecylsalicylic Acid
T638916611-84-0
Anacardic Acid (6-pentadecylsalicylic Acid) is an effective inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.
  • $45
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WM-8014
MOZ-IN-3
T43622055397-18-5
WM-8014 (MOZ-IN-3) is an inhibitor of MOZ(IC50=55 nM), a member of histone acetyltransferases.
  • $52
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SGC-CBP30
T66681613695-14-9
SGC-CBP30 is an effective CREBBP/EP300 inhibitor (IC50: 21/38 nM).
  • $45
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Remodelin hydrobromide
Remodelin HBR, Remodelin
T61331622921-15-6
Remodelin hydrobromide (Remodelin HBR) is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.
  • $34
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JG-2016
T820082887480-87-5
JG-2016, as a small molecule histone acetyltransferase 1 (HAT1) inhibitor, inhibits the growth of human cancer cell lines, inhibits enzyme activity in cellulose, and interferes with tumor growth.
  • $64
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CBL0137
Curaxin 137, CBLC137
T41261197996-80-7
CBL0137 (Curaxin 137), a metabolically stable curaxin, activates p53 (EC50: 0.37 μM) and inhibits NF-κB (EC50: 0.47 μM). It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates the efficacy of gemcitabine in preClinicalal models of pancreatic cancer.
  • $44
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CBP/p300-IN-3
P300/CBP-IN-3
T123452299226-01-8
CBP/p300-IN-3 (P300/CBP-IN-3) is an inhibitor of p300/CBP histone acetyltransferase.
  • $84
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Procyanidin B3
TN115023567-23-9
Procyanidin B3(B3) is a procyanidin dimer that is widely studied due to its high abundance in the human diet and antioxidant activity.
  • $46
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MC4033
T7815628532-21-0
MC4033 is a selective lysine acetyltransferase 8 (KAT8) inhibitor (IC50: 12.1 μM) with anticancer effects, induces apoptosis, and can be used for the study of non-small cell lung cancer.
  • $31
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CPTH2
T8344357649-93-5
CPTH2 is a histone acetyltransferase inhibitor modulating Gcn5 network.
  • $44
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JQAD1
T411802417097-18-6
JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC®; DC50≤ 31.6 nM); comprises an EP300 inhibitor, A485, joined by a linker to a cereblon E3 ligase ligand. JQAD1 brings about degradation of EP300 in neuroblastoma cell lines in a proteasome-dependent manner. JQAD1 suppresses both H3K27ac and EP300 expression levels and induces apoptosis. JQAD1 suppresses tumors growth in NSG mice xenografted with Kelly cells. CRC and MYCN genes are downregulated in tumors treated with JQAD1. JQAD1 exhibits no significant effect on coactivator CBP at concentrations inducing EP300 degradation.
  • $123
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