Tubulysin D 是从粘细菌 Archangium geophyra 和 Angiococcus 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。
CAS：309935-57-7
分子式：C43H65N5O9S
分子量：828.07
纯度：98%
存储：Store at -20°C

Background:

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: 1.7 μM (Tubulin)[1]

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].

[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.