S-Trityl-L-cysteine (NSC 83265) 是一种选择性的别构驱动蛋白 Eg5 抑制剂,抑制基础 ATPase 活性的 IC50 为 1 μM,抑制微管激活的 ATPase 活性的 IC50 为 140 nM。 S-三苯甲基-L-半胱氨酸具有抗肿瘤活性。
Cas No. | 2799-07-7 |
别名 | NSC 83265; S-Tritylcysteine; 3-Tritylthio-L-alanine |
Canonical SMILES | N[C@H](C(O)=O)CSC(C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3 |
分子式 | C22H21NO2S |
分子量 | 363.5 |
溶解度 | DMSO: slightly soluble,Methanol: 1 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 |
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描述 | S-trityl-L-Cysteine is a non-natural amino acid and an inhibitor of Eg5, also known as KSP and Kif11, a mitotic kinesin necessary for mitotic spindle formation. S-trityl-L-Cysteine inhibits the ATPase activity of Eg5 in basal and microtubule-stimulated states (IC50s = 1,000 and 140 nM, respectively). It is selective for Eg5 over nine other human kinesins in an enzyme-coupled assay. It reversibly inhibits Eg5-driven microtubule sliding velocity with an IC50 value of 500 nM using X. laevis recombinant Eg5. It induces cell cycle arrest in HeLa cells (IC50 = 700 nM), reversibly halting the cell cycle in the mitotic phase by inhibiting the separation of duplicated chromosomes and preventing bipolar spindle formation. S-trityl-L-Cysteine inhibits the growth of cancer cells in vitro when tested against the National Cancer Institute (NCI) 60 human cancer cell line panel (average GI50 = 1.3 µM) and in mouse xenograft models. |