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IPA-3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
IPA-3图片
CAS NO:42521-82-4
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
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25mg电议
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产品介绍
理化性质和储存条件
Molecular Weight (MW)350.45
FormulaC20H14O2S2
CAS No.42521-82-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 70 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: 7 mg/mL (20.0 mM)
Other info

Chemical Name: 1,1'-disulfanediylbis(naphthalen-2-ol)

InChi Key: RFAXLXKIAKIUDT-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H14O2S2/c21-17-11-9-13-5-1-3-7-15(13)19(17)23-24-20-16-8-4-2-6-14(16)10-12-18(20)22/h1-12,21-22H

SMILES Code: OC1=CC=C2C=CC=CC2=C1SSC3=C4C=CC=CC4=CC=C3O

Synonyms

IPA-3; IPA 3; IPA3

实验参考方法
In Vitro

In vitro activity: 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. 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.


Kinase Assay: 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.


Cell Assay: 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

In Vivo
Animal model
Formulation & Dosage
References

Chem Biol. 2008 Apr;15(4):322-31; Mol Cancer Ther. 2009 Sep;8(9):2559-65.