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LJ4827

Chemical Structure : LJ4827

CAS No.: 2878445-99-7

LJ4827 (LJ-4827)

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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 331.354
    Formula C13H13N7O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    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

    References

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

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