Tubulysin H (Synonyms: 微管蛋白抑制剂 H)

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Tubulysin H (Synonyms: 微管蛋白抑制剂 H)

Tubulysin H 是具有高细胞毒性的抗微管毒素 (anti-microtubule toxins)，作为 ADC 细胞毒素 (ADC Cytotoxin) 合成 ADC。Tubulysin H 能够从粘细菌 Archangium geophyra 和 Angiococcus disciformis 中分离得到。Tubulysin H 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 H 可抑制微管蛋白 (Microtubule/Tubulin) 聚合并导致细胞周期停滞和凋亡 (apoptosis)。

Tubulysin H Chemical Structure

CAS No. : 799822-09-6

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生物活性	Tubulysin H is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin H can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin H displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC₅₀ values in the low nanomolar range. Tubulysin H inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis^[1]^[2]^[3].
分子量	785.99
Formula	C₄₀H₅₉N₅O₉S
CAS 号	799822-09-6
中文名称	微管蛋白抑制剂 H
结构分类	Ketones, Aldehydes, Acids
初始来源	微生物 Archangium gephyra and Angiococcus disciformis
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.
纯度 & 产品资料	Data Sheet (533 KB) 产品使用指南 (1538 KB)
参考文献	[1]. Steinmetz H, et al. Isolation, crystal and solution structure determination, and biosynthesis of tubulysins–powerful inhibitors of tubulin polymerization from myxobacteria. Angew Chem Int Ed Engl. 2004 Sep 20;43(37):4888-92. [Content Brief] [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. [Content Brief] [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. [Content Brief]

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