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 (4):

Cat. No. Product Name Effect Purity
  • HY-13823
    C646 Inhibitor 98.79%
    C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
  • 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-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-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.