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Cat. No. Product Name CAS No. Information
PC-35580

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.

PC-35579

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.

PC-60499

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.

PC-60498

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.

PC-35322

CPTH2

357649-93-5 CPTH2 is a specific histone acetyltransferase inhibitor modulating Gcn5 network in vitro and in vivo, inhibits H3 acetylation and induces cell-cycle perturbation and apoptosis in U-937 cells; increases E1A CR3 transactivation of human adenovirus through inhibition of HAT GCN5, also reduces virus yield during infection; induces apoptosis and decreases the invasiveness of a ccRCC cell line through the inhibition of KAT3B.
PC-35321

CPTH6 hydrobromide

CPTH6 hydrobromide is a thiazole derivative that can reduce histone acetylation and histone acetyltransferase (HAT) activity in human leukemia cells, CPTH6 is a specific Gcn5/pCAF inhibitor; CPTH6 exerts a significant inhibitory effect on HAT activity of both pCAF and Gcn5, whereas it does not affect p300 and CBP HAT activity; decrease acetylation of histone H3 specifically at lysine 18 in a dose-dependent fashion, does not affect H3 histone methylation at lysines 9 and 4; induces cell-cycle perturbation and apoptosis in AML cells, induces differentiation in AML and neuroblastoma cells; impairs autophagy and reduces autophagosome turnover through an impairment of their degradation pathway.
PC-35320

CPTH6

1099614-81-9 CPTH6 is a thiazole derivative that can reduce histone acetylation and histone acetyltransferase (HAT) activity in human leukemia cells, CPTH6 is a specific Gcn5/pCAF inhibitor; CPTH6 exerts a significant inhibitory effect on HAT activity of both pCAF and Gcn5, whereas it does not affect p300 and CBP HAT activity; decrease acetylation of histone H3 specifically at lysine 18 in a dose-dependent fashion, does not affect H3 histone methylation at lysines 9 and 4; induces cell-cycle perturbation and apoptosis in AML cells, induces differentiation in AML and neuroblastoma cells; impairs autophagy and reduces autophagosome turnover through an impairment of their degradation pathway.

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