Tubulysin M 是一种高度细胞毒性的肽，是从粘细菌 Archangium geophyra 和 Angiococcus disciformis 中分离的。 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，IC50 值在较低的纳摩尔范围内。 Tubulysin M 是一种具有细胞毒性活性微管溶素，抑制微管蛋白聚合并导致细胞周期停滞和凋亡。
CAS：936691-46-2
分子式：C38H57N5O7S
分子量：727.95
纯度：98%
存储：Store at -20°C

Background:

Tubulysin M is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis[1]. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[2]. Tubulysin M is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[3].

[1]. Wang Y, et al. Structural Insights into the Pharmacophore of Vinca Domain Inhibitors of Microtubules. Mol Pharmacol. 2016 Feb;89(2):233-42. [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. [3]. Vlahov IR, et al. Acid mediated formation of an N-acyliminium ion from tubulysins: a new methodology for the synthesis of natural tubulysins and their analogs. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6778-81.