Tubulysin D(Synonyms: 微管蛋白抑制剂 D)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Tubulysin D (Synonyms: 微管蛋白抑制剂 D)

Tubulysin D 是从粘细菌 Archangium geophyraAngiococcus disciformis 中分离的微管溶素中最有效的衍生物。 Tubulysin D 是一种新型四肽,通过抑制微管蛋白聚合而显示出有效的抗肿瘤活性并导致细胞周期停滞和凋亡,IC50 为 1.7 μM。 Tubulysin 在哺乳动物细胞中显示出极其有效的细胞毒活性,包括多药耐药细胞系。

Tubulysin D(Synonyms: 微管蛋白抑制剂 D)

Tubulysin D Chemical Structure

CAS No. : 309935-57-7

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生物活性

Tubulysin D is one of the most potent derivatives among the tubulysins isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin D is a novel tetrapeptide that displays potent antitumor activity and leads to cell cycle arrest and apoptosis by inhibiting tubulin polymerization with an IC50 of 1.7 μM[1]. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[2].

IC50 & Target

IC50: 1.7 μM (Tubulin)[1]

体外研究
(In Vitro)

Tubulysin D has IC50s of 4.7 pM, 3.1 pM, 670 pM and 13 pM for HL60, HCT116, MCF7, A549 cell lines antiproliferative activity, respectively[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

828.07

Formula

C43H65N5O9S

CAS 号

309935-57-7

中文名称

微管蛋白抑制剂 D

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Shibue T, et al. Synthesis and biological evaluation of tubulysin D analogs related to stereoisomers of tubuvaline. Bioorg Med Chem Lett. 2011 Jan 1;21(1):431-4.

    [2]. Kubicek K, et al. The tubulin-bound structure of the antimitotic drug tubulysin. Angew Chem Int Ed Engl. 2010 Jun 28;49(28):4809-12.

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