Tubulysin D |
カタログ番号GC37838 |
チューブリシン D は、粘液細菌種 Archangium geophyra および Angiococcus disciformis から分離されたチューブリシンの中で最も強力な誘導体の 1 つです。チューブリシン D は、強力な抗腫瘍活性を示し、1.7 μM の IC50 でチューブリン重合を阻害することにより、細胞周期停止とアポトーシスをもたらす新規テトラペプチドです。ツブリシンは、多剤耐性細胞株を含む哺乳動物細胞で非常に強力な細胞傷害活性を示し、IC50 値はナノモル範囲未満です。
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Cas No.: 309935-57-7
Sample solution is provided at 25 µL, 10mM.
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.
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