供货周期: | 一周 |
品牌: | 爱必信 |
规格: | >98% |
货号: | abs817908 |
CAS号: | 42521-82-4 |
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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) 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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