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IPA-3

CAS No. : 42521-82-4

MCE 站：IPA-3

产品活性：IPA-3 是一种选择性的，ATP 非竞争的 PAK1 抑制剂，IC₅₀ 值为 2.5 μM，对 PAKs 4-6 没有抑制作用。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton

作用靶点：PAK

In Vitro: 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 ?M, 5 ?M or 20 ?M) 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.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Covalent Screening Library  |  Cytoskeleton Compound Library  |  Fingolimod hydrochloride  |  5-Aminosalicylic Acid  |  FRAX597  |  FRAX486  |  NVS-PAK1-1  |  G-5555  |  GNE 2861  |  FRAX1036  |  LCH-7749944  |  Mesalamine impurity P  |  NVS-PAK1-C

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