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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.

  • Curcumin
    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.
    • $30
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  • Naphthol AS-E
    T785692-78-4
    Naphthol AS-E (nAS-E) is an the KIX-KID interaction and CREB-mediated gene transcription inhibitor.
    • $33
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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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  • 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.
    • $118
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  • CCT077791
    T25215748777-47-1In house
    CCT077791 is a potent inhibitor of p300 and PCAF histone acetyltransferase activity for cancer research.
    • $1,520
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  • Crebinostat
    T270831092061-61-4In house
    Crebinostat is a potent histone deacetylase (HDAC) inhibitor, inhibiting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively.Crebinostat increases the density of synapsin-1 punctae along dendrites in neurons in vitro. Crebinostat increased the density of synapsin-1 punctae along dendrites in neurons in vitro. crebinostat modulated chromatin-mediated neuroplasticity and enhanced memory in mice. crebinostat induced histone H3 and histone H4 acetylation and enhanced the expression of the cAMP-responsive element binding protein (CREB) target gene, Egr1. Crebinostat induces histone H3 and histone H4 acetylation and enhances the expression of Egr1, a cAMP response element binding protein (CREB) target.
    • $350
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  • NEO2734
    T86582081072-29-7In house
    NEO2734 (EP31670) is an orally active and selective inhibitor of p300/CBP and BET bromodomain(IC50 of <30 nM for both p300/CBP and BET bromodomains).
    • $116
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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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    TargetMol | Citations Cited
  • I-CBP112
    T39691640282-31-0
    I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP p300 bromodomains.
    • $51
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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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  • Acetaminophen
    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.
    • $41
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  • CPI-637
    T68111884712-47-3
    CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.
    • $34
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  • NU 9056
    T230951450644-28-6
    NU 9056 is an effective and selective inhibitor of KAT5 histone acetyltransferase with an IC50 of 2 µM. NU 9056 blocks DNA damage response and inhibits protein acetylation in prostate cancer cell lines.
    • $149
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  • Anacardic 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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  • Remodelin
    T3499949912-58-7
    Remodelin is an effective and specific inhibitor of the acetyl-transferase protein NAT10.
    • $50
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    TargetMol | Citations Cited
  • MC4171
    T79086
    MC4171 (compound 34), a selective KAT8 inhibitor (IC50=8.1 µM), demonstrates moderate antiproliferative activity at micromolar concentrations in various cancer cell lines, such as NSCLC and AML. This property highlights its potential utility in cancer research [1].
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  • Garcinol
    T1136678824-30-3
    Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300/CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity. Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 μM and 7.39 μM, respectively.
    • $64
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  • Remodelin hydrobromide
    T61331622921-15-6
    Remodelin hydrobromide (Remodelin HBR) is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.
    • $52
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  • PF-CBP1 hydrochloride
    T32172070014-93-4
    PF-CBP1 hydrochloride (PF-CBP1 HCl) is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.
    • $39
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  • EML 425
    T152161675821-32-5
    EML 425 is a potent and selective inhibitor of CREB binding protein (CBP)/p300 (IC50s: 2.9 and 1.1 μM, respectively).
    • $38
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  • CTPB
    T15014586976-24-1
    CTPB is a potent p300 histone acetyltransferase (HAT) activator that can be used in the preparation of hair growth promoters and or hair loss treatments.
    • $64
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  • DCH36_06
    T9373593273-05-3
    DCH36_06 ((5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione)  as a bona fide is a potent p300 CBP inhibitor
    • $55
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  • L002
    T11807321695-57-2
    L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows potential in the treatment of hypertension‐induced cardiac hypertrophy and fibrogenesis.
    • $34
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  • MOZ-IN-3
    T78815
    MOZ-IN-3 (Compound 6j), a potent KAT6A (MOZ) acetyltransferase inhibitor with an IC50 of 30 nM, exhibits antitumor activity against multiple myeloid leukemia cell lines, including HL-60, U937, SKNO-1, and K562. This compound also demonstrates favorable metabolic stability and pharmacokinetics [1].
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  • MOZ-IN-2
    T120982055397-88-9
    MOZ-IN-2 is an protein MOZ inhibitor(IC50 of 125 μM).
    • $31
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  • A-485
    T140731889279-16-6
    A-485 is a potent and selective catalytic p300/CBP inhibitor(IC50s of 9.8 nM and 2.6 nM for p300 and CBP, respectively).
    • $89
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  • CTX-0124143
    T71832423731-64-0
    CTX-0124143 is a histone acetyltransferase inhibitor with an IC50 value of 1.0 μM for KAT6A.CTX-0124143 can be used to study cellular senescence.
    • $73
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  • PU139
    T28471158093-65-3
    PU139 is a novel inhibitor of histone acetyltransferase (HAT).
    • $56
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  • WM-1119
    T46792055397-28-7
    WM-1119 is a highly potent, selective KAT6A B inhibitor
    • $47
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  • NSC 694623
    T60558907957-34-0
    NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with IC50 of 15.9 μM against recombinant HAT p300/CBP associated factor (PCAF). NSC 694623 shows anti-proliferative activity against some cancer cells, which can be used for anti-cancer research.
    • $43
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  • Histone Acetyltransferase Inhibitor II
    T11563932749-62-7
    Histone Acetyltransferase Inhibitor II is a selective and cell permeable inhibitor of p300 histone acetyltransferase(IC50 : 5 μM).with anti-acetylase activity in mammalian cells.
    • $30
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  • PF-9363
    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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  • NSC 228155
    T6908113104-25-9
    NSC 228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulate EGFR tyrosine phosphorylation.
    • $43
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  • KAT modulator-1
    T791311314006-43-3
    KAT modulator-1 (Compound 3), an epigenetics research tool, selectively interacts with the full-length p300 protein but not its catalytic domain [1].
    • $140
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  • YF-2
    T54681311423-89-8
    YF-2 is blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, CBP, PCAF, and GCN5 with EC50s of 2.75 μM, 29.04 μM and 49.31 μM , respectively
    • $50
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  • CBP/p300-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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  • WM-8014
    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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  • MG 149
    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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  • CPTH2
    T8344357649-93-5
    CPTH2 is a histone acetyltransferase inhibitor modulating Gcn5 network.
    • $31
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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.
    • $43
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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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