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首页-小分子抑制剂&激动剂-Others-Other Targets-Spastazoline
Spastazoline

Chemical Structure : Spastazoline

CAS No.: 2351882-11-4

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Spastazoline (Spastin inhibitor)

货号: PC-36108Not For Human Use, Lab Use Only.

Spastazoline is a potent, selective, cell-permeable, ATP-competitive inhibitor of human Spastin, inhibits the steady-state ATPase activity of the Hs-spastin with IC50 of 99 nM.

规格 价格 库存 数量
10 mg ￥1980 In stock
25 mg ￥3280 In stock
50 mg ￥5280 In stock
100 mg ￥8980 In stock
200 mg Get quote
1 g Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Spastazoline is a potent, selective, cell-permeable, ATP-competitive inhibitor of human Spastin, inhibits the steady-state ATPase activity of the Hs-spastin with IC50 of 99 nM.
Spastazoline does not appreciably inhibit any of the four related AAA proteins (Xl-katanin, Hs-FIGL1, Mm-VCP and Hs-PCH2) at 10 uM, also does not inhibit ATPase activity of recombinant human VPS4.
Spastazoline inhibited Hs-spastin-N386C mutant >100-fold less potently than the wild-type protein; causes a ~2-fold increase in the number of cells with intercellular bridges in treated HeLa-WT cells with spastazoline (4.5h at 10 µM) without effect on the viability and organization of microtubulesof HeLa cell.
Inhibition of spastin activity probably suppresses microtubule severing and thereby impairs spastin dissociation and the loss of ESCRT-III from the sites of membrane constriction; Spastazoline is a valuable probe spastin’s function in dynamic cellular processes.

物理化学性质&存储条件

分子量 382.516
分子式 C20H30N8
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-N-(5-(tert-butyl)-1H-pyrazol-3-yl)-2-(3-isopropylpiperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

参考文献

1. Cupido T, et al. Nat Chem Biol. 2019 Feb 18. doi: 10.1038/s41589-019-0225-6.

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