1. Epigenetics
  2. 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 (17):

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, respectively.
  • HY-N0005
    Curcumin Inhibitor 99.66%
    Curcumin is a natural phenolic compound with impressive antioxidant properties, acts as a p300/CREB-binding protein inhibitor of histone acetyltransferase activity, and also activates nuclear factor (erythroid-2 related) factor 2 (Nrf2).
  • 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-15826
    SGC-CBP30 Inhibitor 99.19%
    SGC-CBP30 is a potent CREBBP/EP300 bromodomain inhibitor with IC50 of 21-69 and 38 nM for CREBBP and EP300 bromodomains, respectively.
  • 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-103669
    HAT-IN-1 Inhibitor
    HAT-IN-1 is an inhibitor of HAT, used in the research of cancer.
  • HY-102060
    MOZ-IN-3 Inhibitor 99.70%
    MOZ-IN-3 is an inhibitor of MOZ, a member of histone acetyltransferases, with an IC50 of 55 nM.
  • 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-15887
    MG 149 Inhibitor 99.48%
    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-19541
    I-CBP112 Inhibitor 98.57%
    I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that targets the CBP/p300 bromodomains.
  • 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-100734
    Histone Acetyltransferase Inhibitor II Inhibitor 99.05%
    Histone Acetyltransferase Inhibitor II, insulin producing cells capable of secreting blood glucose regulating hormones, specially insulin, in response to physiological signals, method of production of said cells and uses thereof.
  • HY-19999A
    PF-CBP1 hydrochloride Inhibitor 99.77%
    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.
  • HY-16706A
    Remodelin hydrobromide Inhibitor 99.16%
    Remodelin HBr salt is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.
  • HY-110263
    EML 425 Inhibitor
    EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.
  • HY-16706
    Remodelin Inhibitor
    Remodelin is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.