Histone Acetyltransferase (HAT)|Inhibitors Agonists Modulators Antagonists|HmoBio.com

Request The Product List ofHistone Acetyltransferase (HAT) Histone Acetyltransferase (HAT)

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.

Cat. No.	Product Name	CAS No.	Information
H9381	NU9056	1450644-28-6	NU9056 is a potent and selective Tip60 (KAT5) histone acetyltransferase inhibitor with an of 2 µM. NU9056 shows >16-fold selectivity for Tip60 over PCAF, p300 and GCN5. NU9056 induces apoptosis of prostate cancer cells.
H8633	iP300w		iP300w is a potent p300/CBP inhibitor.This compound was prepared as a mixture of eight diastereomers. This mixture displayed an IC50 (median inhibitory concentration) of 33 nM versus p300 H3K9Ac in an HTRF (homogeneous time-resolved fluorescence) assay.
H8517	CPI-1612	2374971-81-8	P300/CBP-IN-6 is a p300/CBP histone acetyltransferase (HAT) inhibitor extracted from patent WO2019161162A1, compound 33, has an IC50 of 330 nM for p300 HAT.
H2656	WM-8014	2055397-18-5	WM-8014 (WM8014) is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with Kd of 5 nM and IC50 of 8 nM; WM-8014 is reversible competitor of acetyl coenzyme A and inhibits MYST-catalysed histone acetylation, also inhibits closely related KAT6B (IC50=28 nM), displays >10-fold selectivity over KAT7 and KAT5 (IC50=342 nM and 224 nM), shows no inhibition against KAT8, KAT2A, KAT2B, KAT3A and KAT3B; induces cell cycle exit and cellular senescence without causing DNA damage, reduces acetylation of specific histone lysine residues and changes in gene expression that resemble the genetic loss of KAT6A; selectively reduces liver volume in a zebrafish model of KRASG12V-driven hepatocellular overproliferation, robustly upregulate the cell cycle regulators Cdkn2a and Cdkn1a in hepatocytes.
H2655	WM-1119	2055397-28-7	WM-1119 (WM1119) is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with Kd of 2 nM, shows greate bioavailability and specificity for KAT6A than WM-8014; displays 1,100-fold and 250-fold selectivity over KAT5 and KAT7, respectively; causes cell cycle arrest in G1 and senescence phenotype similar to WM-8014; demonstrates growth inhibition assays in lymphoma cell line EMRK1184 (IC50=0.25 uM, 10-fold potency than WM-8014), increases levels of Cdkn2a and Cdkn2b mRNA and p16INK4a and p19ARF protein, as well as a delayed increase in Cdkn1a mRNA; arrests lymphoma growth in vivo without effect on haematocrit, erythrocytes or platelet numbers.
H2653	Windorphen	19881-70-0	A potent, selective inhibitor of p300 histone acetyltransferase (IC50=4.2 uM); displays >10-fold selectivity over other histone acetyltransferases; inhibits Wnt3a-inducible TOPFLASH-luciferase activity with IC50 of 1.5 uM, exhibits remarkable specificity toward β-catenin-1 function and selectively blocks the Wnt signal required for ventral development; robustly and selectively kills cancer cells that harbor Wnt-activating mutations.
H2652	TTK21	709676-56-2	TTK21 (CBP-p300 activator TTK21) is a small molecule activator of CBP/p300 histone acetyltransferase activity with a maximal effect at a concentration of 275 uM; induces acetylation of histones H3 and H4 in vitro but not H2B and H2A; promotes neurogenesis and extends memory duration in adult mice, promotes regeneration and sprouting of sensory and motor axons, as well as recovery of sensory and motor functions in both the mouse and rat model of spinal cord injury.
H2651	TH1834 dihydrochloride	2108830-09-5	TH1834 dihydrochloride (TH-1834, TH 1834) is a novel potent specific histone acetyltransferase Tip60 inhibitor; induces apoptosis in breast cancer cell lines with more cytotoxicity than staurosporine; increases the γH2AX foci in the cancer cell lines PC-3 and DU-145 combined with IR; induces apoptosis and increases unrepaired DNA damage in breast cancer cells.
H2650	TH1834	2108830-08-4	TH1834 (TH-1834, TH 1834) is a novel potent specific histone acetyltransferase Tip60 inhibitor; induces apoptosis in breast cancer cell lines with more cytotoxicity than staurosporine; increases the γH2AX foci in the cancer cell lines PC-3 and DU-145 combined with IR; induces apoptosis and increases unrepaired DNA damage in breast cancer cells.
H2649	SPV 106	1036939-38-4	SPV 106 is the first mixed activator/inhibitor of Histone acetyltransferases (HATs), potentiates p300/CBP-associated factor (PCAF) HAT activity while inhibiting those of p300/CBP and recombinant CBP; significantly increases the H3 acetylation level in U937 cells, but no detectable effect on the acetylation level of the non-histone substrate a-tubulin; restores normal levels of H3K9Ac and H3K14Ac, reduces DNA CpG hypermethylation, and recovers D-CMSC proliferation and differentiation, enhances memory for fear extinction and prevents fear renewal in mice.

Select Your Country or Region

Request The Product List ofHistone Acetyltransferase (HAT) Histone Acetyltransferase (HAT)

Request The Product List

* Indicates a Required FieldYour information is safe with us.