MC4171 | KAT8 inhibitor | Probechem Biochemicals

Chemical Structure : MC4171

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MC4171 (KAT8 inhibitor 34, MC 4171)

货号: PC-20777Not For Human Use, Lab Use Only.

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.

规格	价格	库存
5 mg	￥1580	In stock
10 mg	￥2480	In stock
25 mg	￥4380	In stock
50 mg	￥7580	In stock
100 mg		Get quote

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生物&药学活性

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.
MC4171 displays high selectivity against a panel of KATs (KAT2A and the MYST family members KAT5, KAT6A, KAT6B, and KAT7), KDACs (KDAC1–3, 6, and 8).
MC4171 exhibits target engagement as stabilizing KAT8 against thermal-induced aggregation in cells.
MC4171 (50 uM) reduces more than 50% reduction of H4K16Ac in HT29 CRC cell line, with no influence on KAT8 expression levels or on H3K27 acetylation (acetylated by KAT3A/B).
MC4171 displayed antiproliferative activity in A549 cells (65% cell proliferation inhibition at 50 uM; 80% cell proliferation inhibition at 100 uM).
MC4171 is cancer-selective, exhibits mid-micromolar antiproliferative activity in different cancer cell lines, including NSCLC and AML, without impacting the viability of nontransformed cells.
MC4171 is valuable chemical tool for elucidating KAT8 biology.

物理化学性质&存储条件

分子量	357.37
分子式	C21H15N3O3
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	(Z)-4-(4-((1H-pyrrol-2-yl)methylene)-5-oxo-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid

参考文献

1. Francesco Fiorentino, et al. Journal of Medicinal Chemistry. May 8, 2023

MC4171 (KAT8 inhibitor 34, MC 4171)

生物&药学活性

物理化学性质&存储条件

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MC4171 (KAT8 inhibitor 34, MC 4171)

生物&药学活性

物理化学性质&存储条件

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