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 (40):

Cat. No. Product Name Effect Purity
  • HY-107455
    A-485 Inhibitor 99.90%
    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[1].
  • HY-N0005
    Curcumin Inhibitor
    Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
  • HY-66005
    Acetaminophen 99.96%
    Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent[1][2][3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[4].
  • 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[1].
  • 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-136938
    NEO2734 Inhibitor 99.66%
    NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains[1]. NEO2734 is active in SPOP mutant and wild-type prostate cancer[2].
  • HY-136285
    CPI-1612 Inhibitor
    CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC50 of 8.1 nM for EP300 HAT. CPI-1612 has an anticancer activity[1].
  • HY-124960
    CTPB Activator >99.0%
    CTPB is a good activator of p300 histone acetyl transferase (HAT) enzyme[1].
  • HY-102058
    WM-1119 Inhibitor 98.09%
    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[1].
  • HY-15826
    SGC-CBP30 Inhibitor 99.83%
    SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects[1][2][3].
  • HY-16706A
    Remodelin hydrobromide Inhibitor 99.49%
    Remodelin, a specific inhibitor of N-acetyltransferase NAT10, can ameliorate Hutchinson-Gilford Progeria Syndrom (HGPS) cellular phenotypes. Remodelin acts in a progerin- and FTI-independent pathway, by targeting and inhibiting NAT10[1]. NAT10 is a protein with histone acetylation activity and primarily identified to be involved in regulation of telomerase activity[2].
  • HY-15887
    MG 149 Inhibitor 99.07%
    MG149 (Tip60 HAT inhibitor) 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)[1].
  • HY-100482
    CPI-637 Inhibitor 99.94%
    CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP[1].
  • HY-108696
    GNE-781 Inhibitor 98.19%
    GNE-781 is an orally active, 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. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model[1].
  • HY-108435
    GNE-049 Inhibitor 98.98%
    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[1].
  • 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[1]. 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[2].
  • HY-100726
    GNE-272 99.74%
    GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300[1].
  • 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-107569
    Garcinol Inhibitor >98.0%
    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[1]. 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[2].
  • HY-19541
    I-CBP112 Activator 98.40%
    I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.