RGNCY-0055 (SR31527 KIFC1 inhibitor)

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SR31527 is an inhibitor of Kinesin-like protein KIFC1.  KIFC1 plays a critical role in centrosome clustering in cancer cells but not not essential for normal cells.  SR31527 inhibited microtubule-stimulated KIFC1 ATPase activity (IC50 = 6.6 mM) and bound directly to KIFC1 with high affinity at a novel allosteric site.  SR31527 prevented bipolar clustering of extra-centrosomes in triple negative breast cancer (TNBC) cells and significantly reduced its cell colony formation and viability.  It was however, shown to be less toxic to normal cells and fibroblasts.  SR31527 maybe a potential lead for the development of new therapeutic agents for breast cancer.

Systematic Name: 5-amino-3-(4-methoxyphenyl)-2-phenyl-1,2,4-thiadiazol-2-ium


Formula: C15H14N3OS+

Mol Wt: 284.36

PMID:  26846349

Tags: Cancer, small molecule, breast cancer, KIFC1, centrosomes, RGNCY-0055