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首页-小分子抑制剂&激动剂-Epigenetics-Histone Acetyltransferase (HAT)-CHI-KAT8i5
CHI-KAT8i5

Chemical Structure : CHI-KAT8i5

CAS No.: 2839860-29-4

CHI-KAT8i5

货号: PC-23724Not For Human Use, Lab Use Only.

CHI-KAT8i5 is a specific small molecule inhibitor of KAT8 (lysine acetyltransferase 8), directly binds to KAT8 with SPR KD of 19.72 uM, suppresses esophageal squamous cell carcinoma (ESCC) growth through targeting KAT8/c-Myc signaling pathway.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CHI-KAT8i5 is a specific small molecule inhibitor of KAT8 (lysine acetyltransferase 8), directly binds to KAT8 with SPR KD of 19.72 uM, suppresses esophageal squamous cell carcinoma (ESCC) growth through targeting KAT8/c-Myc signaling pathway.
CHI-KAT8i5 suppresses ESCC cell proliferation (IC50=2-3 uM) through the inhibition of KAT8 lysine acetyltransferase activity.
CHI-KAT8i5 does not bind to other proteins in HAT family (KAT2A, KAT2B, KAT5, and KAT7).
CHI-KAT8i5 could significantly inhibit KYSE 30 and KYSE 150 clone formation, 5 and 15 μM CHI-KAT8i5 induces cancer cell apoptosis in a dose-dependent manner.
CHI-KAT8i5 (2-15 uM) dose-dependently decreases H4K16ace and c-Myc in KYSE30 cells, suppresses NPM1 and PPAT transcript expression in ESCC cell lines.
CHI-KAT8i5 (50 or 200 mg/kg) suppresses ESCC tumor growth in patient-derived ESCC xenografts.

物理化学性质&存储条件

分子量 523.68
分子式 C23H29N3O5S3
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

2-(4-(N,N-diethylsulfamoyl)-3-hydroxystyryl)-N,N-diethylbenzo[d]thiazole-6-sulfonamide

参考文献

1. Zhang D, et al. Cell Rep. 2025 Jan 7;44(1):115135.

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