IPA-3

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抑制剂描述：

产品名称：IPA-3

产品别名：见爱必信官网

英文别名：IPA-3

靶点：PAK

CAS：42521-82-4

纯度：＞98%

外观：见爱必信官网

保存方法：Store at -20°C

描述：

IPA-3是非ATP竞争的PAK1选择性抑制剂，IC50为2.5 μM，对于II型 PAKs (PAKs 4-6)无抑制活性。

溶解性：DMSO : 65 mg/mL (185.5 mM)
Ethanol : 7 mg/mL (19.97 mM)

体外研究：

IPA-3 inhibits Pak1 activation in part by binding covalently to the regulatory domain of Pak1. IPA-3 binds Pak1 covalently in a time- and temperature-dependent manner. IPA-3 prevents binding of the Pak1 activator Cdc42. IPA-3 binds directly to the Pak1 autoregulatory domain. IPA-3 reversibly inhibits PMA-induced membrane ruffling in cells. IPA-3 (2 μM, 5 μM or 20 μM) reduces cell spreading in human primary Schwann and schwannoma cells. IPA-3 treatment significantly reduces the number of adherent Schwann and schwannoma cells in a dose-dependent manner. IPA-3 is a non ATP-competitive, allosteric inhibitor of p21-activated kinase 1 (Pak1). PIR3.5 is the control compound of IPA-3. IPA-3 prevents Cdc42-stimulated Pak1 autophosphorylation on Thr423. IPA-3 also prevents sphingosine-dependent Pak1 autophosphorylation. IPA-3 does not target exposed cysteine residues on Pak1. The disulfide bond of IPA-3 is critical for inhibition of Pak1 and in vitro reduction by the reducing agent dithiothreitol (DTT) abolishes Pak1 inhibition by IPA-3. IPA-3 inhibits activation of Pak1 by diverse activators, but does not inhibit preactivated Pak1. IPA-3 inhibits PDGF-stimulated Pak activation in mouse embryonic fibroblasts.

体内研究：

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