Chemical Structure : MU1920
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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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.
分子量 | 321.40 | |
分子式 | C17H15N5S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Martín Moyano P, et al. Angew Chem Int Ed Engl. 2024 Nov 6:e202412786.
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