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Chemical Structure : LJ4827
Catalog No.: 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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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.
| M.Wt | 331.354 | |
| Formula | C13H13N7O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Eun-Ji Kwon, et al. Cancer Res (2022) 82 (12_Supplement): 3949.
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