AZ82

An inhibitor of KIFC1

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库存: 现货

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1mg

￥512.00

410.00

- +
5mg

￥2825.00

2260.00

- +
10mg

￥4262.00

3410.00

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25mg

￥8525.00

6820.00

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货号: ajci22154
CAS: 1449578-65-7
别名:
分子式: C28H31F3N4O3S
分子量: 560.6
纯度: >98%
溶解度: DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 20 mg/ml,Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
储存: Store at -20°C
库存: 现货

Background

AZ82 is a small molecule inhibitor of KIFC1/HSET, a kinesin-14 family protein that is important for assembling bipolar spindles in cancer cells containing supernumerary centrosomes.[1]? AZ82 binds to the KIFC1/microtubule complex and inhibits its microtubule-stimulated activity (IC50 = 300 nM) in an ATP-competitive (Ki = 43 nM) and microtubule-noncompetitive manner but does not inhibit basal KIFC1 activity at a concentration of 100 uM. [2] It is selective for KIFC1 over a panel of nine kinesin motor proteins at a concentration of 5 uM. AZ82 induces multipolar spindle formation in cancer cell lines with high (BT549), but not low (HeLa and MCF-7), numbers of extra chromosomes.

Reference:
[1]. Godinho, S.A., and Pellman, D. Causes and consequences of centrosome abnormalities in cancer. Philos. Trans. R. Soc. Lond. B Biol. Sci. 369(1650), pii: 20130467 (2014).
[2]. Wu, J., Mikule, K., Wang, W., et al. Discovery and mechanistic study of a small molecule inhibitor for motor protein KIFC1. ACS Chem. Biol. 8(10), 2201-2208 (2013).