AZ82 是一种选择性驱动蛋白样蛋白 KIFC1 (HSET/KIFC1) 抑制剂，对 KIFC1 的 Ki 为 43 nM，IC50 为 300 nM。
| Cas No. | 1449578-65-7 |
| 化学名 | αR-[[(5-methyl-4-propyl-2-thienyl)carbonyl]amino]-N-(3R)-3-pyrrolidinyl-6-[3-(trifluoromethoxy)phenyl]-3-pyridinepropanamide |
| Canonical SMILES | O=C(N[C@@H]1CCNC1)[C@H](NC(C2=CC(CCC)=C(C)S2)=O)CC3=CC=C(C4=CC(OC(F)(F)F)=CC=C4)N=C3 |
| 分子式 | C28H31F3N4O3S |
| 分子量 | 560.6 |
| 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 |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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). |
