GSK-923295 | CAS:1088965-37-0

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Name:GSK-923295; 
Cat. No. :CS-0056
CAS No. :1088965-37-0
Formula:C32H38ClN5O4
M. Wt. : 592.13
Solubility:10 mM in DMSO

GSK-923295 is a special, allosteric inhibitor of CENP-E kinesin motor ATPase activity, with Ki of 3.2±0.2 nM and 1.6± 0.1 nM for human and canine, respectively.IC50 & Target: Ki: 3.2 nM (human CENP-E), 1.6 nM (canine CENP-E)[1]In Vitro: GSK-923295 (GSK923295) is a first-in-class, specific, allosteric inhibitor of CENP-E kinesin motor function. GSK923295 is uncompetitive with both ATP and MT, inhibiting CENP-E MT-stimulated ATPase activity with a Ki of 3.2±0.2 nM and 1.6±0.1 nM for human and canine, respectively. GSK923295 inhibits release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules[1]. GSK923295 has broad growth inhibitory activity in a panel of 237 cancer cell lines and produces significant tumor growth-delay in 8 of the 11 mouse xenograft tumor models with IC50s of 17.2 nM, 55.6 nM, 42 nM, and 51.9 nM for SW48, RKO (BRAF mutant), SW620 (KRAS mutant), and HCT116 (KRAS mutant), respectively[2]. GSK923295 is a potent and selective small molecule inhibitor of human CENPE with a Ki of 3.2 nM. GSK923295 demonstrates broad efficacy against a panel of 19 human neuroblastoma derived cell lines with an average growth IC50 of 41 nM[3].In Vivo: Xenografts of mice treated with GSK-923295 (GSK923295) shows significant tumor growth delay compared to the control arm (NB-EBc1 p[3].

Wood KW, et al. Antitumor activity of an allosteric inhibitor of centromere-associated protein-E. Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44. Balamuth NJ, et al. Serial transcriptome analysis and cross-species integration identifies centromere-associated protein E as a novel neuroblastoma target. Cancer Res. 2010 Apr 1;70(7):2749-58. Mayes PA, et al. Mitogen-activated protein kinase (MEK/ERK) inhibition sensitizes cancer cells to centromere-associated protein E (CENP-E) inhibition. Int J Cancer. 2013 Feb 1;132(3):E149-57.