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首页-小分子抑制剂&激动剂-Epigenetics-Histone Acetyltransferase (HAT)-BAY-184
BAY-184

Chemical Structure : BAY-184

CAS No.: 2520347-03-7

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BAY-184 (BAY184)

货号: PC-23297Not For Human Use, Lab Use Only.

BAY-184 is a potent, selective and in vivo-active KAT6A/B inhibitor with IC50 of 71/83 nM respectively.

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5 mg ￥2880 In stock
10 mg ￥4580 In stock
25 mg ￥7580 In stock
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纯度 & COA & 质检文件 纯度: 98.7% (HPLC) Select Batch:

生物&药学活性

BAY-184 is a potent, selective and in vivo-active KAT6A/B inhibitor with IC50 of 71/83 nM respectively.
BAY-184 displays an overall good selectivity, with high selectivity against the close members of the MYST family, with only a residual low micromolar activity for KAT7 (11-fold), and with no activity against the more distantly related histone acetyltransferase p300 (IC50 > 10 μM).
BAY-184 also shows high selectivity against a full kinase panel at a concentration of 10 μM (366 kinases) at Eurofins.
BAY-184 (1 uM) elicited a swift decline in H3K23ac levels in ZR-75-1 cells, shows IC50 of 670 nM for H3K23 acetylation in HTRF assays, and IC50 of 168 nM in ER target gene reporter assay.
BAY-184 inhibits cell growth of ZR-75-1 breast cancer cells with IC50 of 130 nM, shows IC50 values of <1 uM against ER-positive breast cancer subtypes.
BAY-184 (50-150 mg/kg, po, twice daily (2 qd)) induced a dose-dependent inhibition of tumor growth in ZR-75-1 xenografts.

物理化学性质&存储条件

分子量 420.48
分子式 C23H20N2O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-([1,1'-Biphenyl]-2-sulfonyl)-6-(dimethylamino)-1-benzofuran-2-carboxamide

参考文献

1. Ter Laak A, et al. J Med Chem. 2024 Oct 25. doi: 10.1021/acs.jmedchem.4c01709.

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