S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC 50 of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities.
性状
Solid
IC50 & Target[1][2]
Eg5
体外研究(In Vitro)
S-Trityl-L-cysteine binds to a unique pocket in the Eg5 motor domain formed by secondary structural elements (helix a2/loop L5/helix a3).S-Trityl-L-cysteine (1-20 μM; for 72 h) could mediate cell apoptosis, as well as cell cycle arrest, in a dose-dependent manner. S-Trityl-L-cysteine-mediated apoptosis and cell cycle arrest were triggered by activation of the mitogen-activated protein kinase and nuclear factor kB signaling pathways.S-Trityl-L-cysteine induces mitotic arrest in HeLa cells (IC50 of 700 nM) with characteristic monoastral spindles. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Wei Wu, et al. S-trityl-L-cysteine, a novel Eg5 inhibitor, is a potent chemotherapeutic strategy in neuroblastoma. Oncol Lett. 2018 Jul;16(1):1023-1030. [2]. Salvatore DeBonis, et al. In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities. Mol Cancer Ther. 2004 Sep;3(9):1079-90.
溶解度数据
In Vitro: DMSO : 25 mg/mL (68.78 mM; Need ultrasonic)配制储备液