IPA-3 |
Catalog No.GC16225 |
IPA-3은 IC50이 2.5μM인 선택적 비 ATP 경쟁적 PAK1 억제제이며 그룹 II PAK(PAK 4-6)에 대한 억제를 나타내지 않습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 42521-82-4
Sample solution is provided at 25 µL, 10mM.
IPA-3 is an autoregulatory domain inhibitor of p21-activated kinase (Pak) with IC50 value of 2.5μM [1].
IPA-3 is a highly selective and non-ATP-competitive inhibitor that targets the autoregulatory mechanism of group I Paks. IPA-3 is screened out as an inhibitor of Pak1 by measuring ATP hydrolysis. In the in vitro assays, IPA-3 inhibits Pak1 autophosphorylation stimulated by Cdc42 or sphingosine. It shows an IC50 value of 2.5μM in the kinase assay. This inhibition of Pak1 is reported to be noncompetitive with ATP. Besides that, IPA-3 is found to remarkably inhibit the kinase activity of other group I Pak members, Pak2 and 3 at concentration of 10μM. Furthermore, 30μM IPA-3 can prevent both basal and PDGF-stimulated Pak activities in mouse embryonic fibroblasts [1].
References:
[1] Deacon S W, Beeser A, Fukui J A, et al. An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase. Chemistry & biology, 2008, 15(4): 322-331.
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