1. Signaling Pathways
  2. Epigenetics
  3. Histone Acetyltransferase

Histone Acetyltransferase

The histone acetyltransferase (HAT) enzymes p300 and CBP are closely related paralogs that serve as transcriptional coactivators. The p300 and CBP catalyze the acetylation of Lys residues in histones and other proteins. Serving as transcriptional coactivators, p300 and CBP participate in numerous ways to regulate cell growth, differentiation, and gene expression across many organ systems and physiologic pathways. Dysregulation of p300/CBP by mutation, altered expression, or other mechanisms has been linked to disease states, including various malignancies such as acute leukemias and prostate cancer. Furthermore, p300/CBP is critical in development as evidenced by the genetic disorder Rubinstein-Taybi syndrome, which occurs with loss of function mutations in single alleles of either p300 or CBP.

Inhibitors of p300/CBP HAT activity have been developed and are under investigation as therapeutics for a number of diseases.

Histone Acetyltransferase Related Products (30):

Cat. No. Product Name Effect Purity
  • HY-107455
    A-485 Inhibitor 99.08%
    A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively.
  • HY-N0005
    Curcumin Inhibitor 99.66%
    Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
  • HY-13823
    C646 Inhibitor >98.0%
    C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
  • HY-100482
    CPI-637 Inhibitor 99.94%
    CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.
  • HY-102058
    WM-1119 Inhibitor >98.0%
    WM-1119 is a highly potent and selective KAT6A inhibitor, with an IC50 of 0.25 μM for KAT6A in lymphoma cells, the binding KD values of WM-1119 with KAT6A, KAT5 and KAT7 are 2 nM, 2.2 μM, 0.5 μM , respectively.
  • HY-101084
    NSC 228155 Inhibitor >98.0%
    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.
  • HY-16531
    YF-2 Activator 99.36%
    YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
  • HY-124960
    CTPB Activator
    CTPB is a good activator of p300 histone acetyl transferase (HAT) enzyme.
  • HY-N2020
    Anacardic Acid Inhibitor >98.0%
    Anacardic Acid, extracted from cashew nut shell liquid, is a histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC50s of ∼8.5 μM and ∼5 μM, respectively.
  • HY-100726
    GNE-272 >98.0%
    GNE-272 is a potent and selective in vivo probe for the bromodomains of CBP/EP300 with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively.
  • HY-15826
    SGC-CBP30 Inhibitor 99.74%
    SGC-CBP30 is a potent CREBBP/EP300 bromodomain inhibitor with IC50 of 21-69 and 38 nM for CREBBP and EP300 bromodomains, respectively.
  • HY-15887
    MG 149 Inhibitor 99.07%
    MG149 is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF(IC50= 47 uM); little potent for PCAF and p300(IC50 >200 uM).
  • HY-16706A
    Remodelin hydrobromide Inhibitor 99.16%
    Remodelin hydrobromide is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.
  • HY-102060
    WM-8014 Inhibitor 99.70%
    WM-8014 is an inhibitor of MOZ, a member of histone acetyltransferases, with an IC50 of 55 nM.
  • HY-108696
    GNE-781 Inhibitor 98.19%
    GNE-781 is a highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively.
  • HY-19541
    I-CBP112 Activator 98.57%
    I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.
  • HY-108435
    GNE-049 Inhibitor 99.33%
    GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.
  • HY-100734
    Histone Acetyltransferase Inhibitor II Inhibitor 99.05%
    Histone Acetyltransferase Inhibitor II is a potent and cell permeable p300 inhibitor, with an IC50 of 5 µM; Histone Acetyltransferase Inhibitor II can be used in cancer research.
  • HY-19999A
    PF-CBP1 hydrochloride Inhibitor 99.85%
    PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain.
  • HY-100697
    TPOP146 Inhibitor 99.66%
    TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
Isoform Specific Products

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