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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Haspin Kinase-MU1920
MU1920

Chemical Structure : MU1920

CAS No.:

MU1920 (MU 1920)

货号: PC-23393Not For Human Use, Lab Use Only.

MU1920 is a potent, highly selective inhibitor of haspin kinase with IC50 of 6 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MU1920 is a potent, highly selective inhibitor of haspin kinase with IC50 of 6 nM.
MU1920 significant selectivity against the off-target kinases CDKL3, CDKL4, CLK2, DYRK2, PIM1, TAF1L and TRB2.
MU1920 elicits efficient inhibition of Haspin (with the IC50 values of 0.13 uM for HeLa and 0.35 uM forMDA-MB-231), indicated by the absence of phosphorylation ofThr3 in histone H3 (specific target of Haspin) as determined bywestern blot.
MU1920 shows ellular inhibition of Haspin by the ELISA assay in coloncarcinoma cell line HT29, with IC50 value of 94 nM.
MU1920 does not affect the viability inlarge panel of 160 cancer cell lines (EC50 >50 uM).
MU1920 is good with the oral bioavailability 53% at the 20 mpk dose, is well tolerated (no signs of acute toxicity were observed in the animals) at 100 mpk dose.

物理化学性质&存储条件

分子量 321.40
分子式 C17H15N5S
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-(1,4-dimethyl-1H-pyrazol-3-yl)-3-(pyridin-4-yl)thieno[3,2-b]pyridin-5-amine

参考文献

1. Martín Moyano P, et al. Angew Chem Int Ed Engl. 2024 Nov 6:e202412786.

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