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.

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.

NiCur is a potent and selective CBP HAT inhibitor with an IC50 value of 0.35 μΜ. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins.

CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B).

CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol.

ENL YEATS Domain inhibitor 7 is a selective, small molecule inhibitor of ENL YEATS Domain with IC50 of 0.62 uM in inhibiting the ENL-acetyl-H3 interaction.ENL YEATS Domain inhibitor 7 displayed strong selectivity toward the ENL YEATS domain over all other human YEATS domains.ENL YEATS Domain inhibitor 7 exhibited on-target inhibition of ENL in cultured cells and a synergistic effect with the bromodomain and extraterminal domain inhibitor JQ1 in killing leukemia cells.

IMP-1575 (IMP1575) is a potent, selective Hedgehog acyltransferase (HHAT) inhibitor with Ki/IC50 of 38 nM/0.75 uM (Acyl-cLIP assay).IMP-1575 is the first sub-micromolar small-molecule HHAT inhibitor reported to-date.IMP‐1575 (50-0.023 μM) was therefore analyzed for effects on HHAT kinetics at varying Pal‐CoA concentrations (50–0.19 μM).IMP-1575 is a chemical tool and methodology to provide insight into HHAT which may expedite future studies and drug discovery efforts against this important target class.

Coumarin-SAHA is a fluorescent probe for determining the binding affinities (kd) and the dissociation off-rates (koff) of the HDAC8-inhibitor complexes.

DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC50 values of 0.040, 0.15, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. DS17701585 can be used for cancer research.

EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively.

B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines.

DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research.

JG-2016 is a small molecule inhibitor of histone acetyltransferase 1 (HAT1) with IC50 of 14.8 uM in the HAT1 acetylation assays.

MC4171 (KAT8 inhibitor 34) is a first-in-class, selective and reversible lysine acetyltransferase KAT8 inhibitor with IC50 of 8.1 uM and SPR Kd of 2.04 uM.