LJ4827 | Haspin inhibitor | Probechem Biochemicals

Chemical Structure : LJ4827

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LJ4827 (LJ-4827)

货号: PC-49320Not For Human Use, Lab Use Only.

LJ4827 (LJ-4827) is a potent, specific inhibitor of HASPIN, a mitotic kinase for Histone H3, with Ki value of 0.46 nM, enzyme IC50 of 0.155 nM in HASPIN kinase assay performed with Histone H3 peptide.

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生物&药学活性

LJ4827 (LJ-4827) is a potent, specific inhibitor of HASPIN, a mitotic kinase for Histone H3, with Ki value of 0.46 nM, enzyme IC50 of 0.155 nM in HASPIN kinase assay performed with Histone H3 peptide.
LJ4827 displays excellent selectivity against a panel of 468 kinases (403 non-mutant and 65 mutant kinases) at 100 nM, with 3 kinases CLK2, DYRK1A (in the GMGC group), MEK5 (in the STE group) exception.
LJ4827 efficiently delayed mitotic progression without double strand break (DSB) unlike 5ITU and significantly attenuated Aurora B localization at centromere in cancer cell lines with high expression of HASPIN.
LJ4827 deomstarted the synthetic lethal effect of cotreatment with chemical inhibitor of BUB1, PLK1 or AURKA.

物理化学性质&存储条件

分子量	331.354
分子式	C13H13N7O2S
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	(2R,3R,4S,5R)-2-(4-amino-5-ethynyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-(azidomethyl)tetrahydrothiophene-3,4-diol

参考文献

1. Eun-Ji Kwon, et al. Cancer Res (2022) 82 (12_Supplement): 3949.

LJ4827 (LJ-4827)

生物&药学活性

物理化学性质&存储条件

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LJ4827 (LJ-4827)

生物&药学活性

物理化学性质&存储条件

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