CAS:2351882-11-4(R)-N-(5-(tert-Butyl)-1H-pyrazol-3-yl)-2-(3-isopropylpiperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

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Spastazoline is a potent and selective spastin (a microtubule-severing AAA protein) inhibitor, with an IC50 of 99 nM for human spastin.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

2351882-11-4

储存条件

分子式

C20H30N8

运输

蓝冰

分子量

382.51

别名

溶解度

DMSO	95.0 mg/mL (248.4 mM) warming

动物实验配方

生物活性

描述The AAA superfamily (ATPases associated with diverse cellular activities) has been linked to a wide range of cellular processes, including cell division, cytoskeleton organization, and organelle biogenesis. Spastin is a microtubule-severing AAA protein needed for cell division and intracellular vesicle transport. Chemical probes that inhibit their activities in cells on similarly fast timescales can be valuable tools to dissect dynamic mechanisms. Spastazoline is a potent and selective cell-permeable probe for spastin with an IC₅₀ of 99 ± 18 nM for human spastin. Treating HeLa-WT cells with spastazoline for 4.5 hours (10 µM) resulted in a ~2-fold increase in the number of cells with intercellular bridges compared to DMSO control indicating that spastazoline inhibits intercellular bridge disassembly by interfering with spastin activity. In dividing HeLa-WT cells treated with Spastazoline, EGFP-spastin accumulated at chromatin within 2–4 min after cleavage furrow ingression initiation. Imaging HeLa-WT cells in anaphase treated with spastazoline (10 µM for 1 hour) also revealed GFP-spastin puncta on chromosomes^[1].