A novel potent specific histone acetyltransferaseTip60 inhibitor.

A novel potent specific histone acetyltransferaseTip60 inhibitor.

A potent, selective and, cell and in vivo active p300/CBP catalytic inhibitor with IC50 of 9.8/2.6 nM.

Anacardic acid inhibits the histone acetyltransferase (HAT) activity of the transcription co-activators p300 and p300/CREB-binding protein-associated factor (pCAF) with IC50 values of 8.5 and 5 µM, respectively.

C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM. Preferentially selective for p300 versus other acetyltransferases.

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.

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 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.

I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.142 and 0.625 μM, respectively).

L002 is a p300 inhibitor (IC50=1.98 μM) that inhibits p53 and histone acetylation. Suppresses STAT3 activation in vitro and suppresses tumor growth in some mouse cell lines.

MG 149 is an inhibitor of histone acetyltransferases (HAT) with IC50 values of 74μM and 47μM for Tip60 and MOF, respectively.

WM-1119(WM1119) is a highly potent, selective inhibitors of KAT6A and KAT6B.

WM-8014(WM8014) is a highly potent, selective inhibitors of KAT6A and KAT6B.

YF2 is a First-in-Class Histone Acetyltransferase (HAT) Activators for Precision Targeting of Epigenetic Derangements in Lymphoma.

OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells.

Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation.

DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors.

MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM.

UNC2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM.

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.

AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.

DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.