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GSK923295

Chemical Structure : GSK923295

CAS No.: 1088965-37-0

GSK923295 (GSK-923295)

Catalog No.: PC-42514Not For Human Use, Lab Use Only.

GSK-923295 (GSK923295) is the first potent, allosteric inhibitor of CENP-E kinesin motor ATPase activity with Ki of 3.2 nM.

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Biological Activity

GSK-923295 (GSK923295) is the first potent, allosteric inhibitor of CENP-E kinesin motor ATPase activity with Ki of 3.2 nM.
GSK-923295 shows excellent selectivity against a panel of mitotic human kinesins.
GSK-923295 exhibits inhibition of cell proliferation in a broad panel of human cancer cell lines and induces mitotic arrest leading to apoptosis and cell death (SKOV-3 IC50=22 nM; Colo205 IC50=22 nM).
GSK-923295 induces tumor regressions in vivo.

Physicochemical Properties

M.Wt 592.1282
Formula C32H38ClN5O4
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

Benzamide, 3-chloro-N-[(1S)-2-[[2-(dimethylamino)acetyl]amino]-1-[[4-[8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl]phenyl]methyl]ethyl]-4-(1-methylethoxy)-

References

1. Wood KW, et al. Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44.

2. Qian X, et al. ACS Med Chem Lett. 2010 Jan 19;1(1):30-4.

3. Balamuth NJ, et al. Cancer Res. 2010 Apr 1;70(7):2749-58.

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