IPA-3
目录号: PL08766 纯度: ≥99%
CAS No. :42521-82-4
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中文名称
IPA-3
中文别名
二(2-羟基-1-萘基)二硫醚;IPA-3
英文名称
IPA-3
英文别名
1-[(2-hydroxynaphthalen-1-yl)disulfanyl]naphthalen-2-ol;1-[(2-hydroxynaphthyl)disulfanyl]naphthalen-2-ol;CHEMBL472940;F0400-0044;bis-(2-hydroxy-1-naphthyl)disulphide;1,1'-Disulfandiyl-di-[2]naphthol;UNII-3XFG6MQ9G2;Bis-(2-hydroxy-naphthyl-(1))-disulfid;[14C]-IPA-3;1,1'-disulfanediyl-di-[2]naphthol;1,1'-Dithiodi-2-naphthol;2.2'-Dioxy-(1.1'-dinaphthyl-disulfid);IPA 3;IPA-3;1,1′-Disulfanediyldinaphthalen-2-ol
Cas No.
42521-82-4
分子式
C20H14O2S2
分子量
350.45
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC 50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).
性状
Solid
IC50 & Target[1][2]
PAK1 2.5 μM (IC50)
体外研究(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 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 disulf
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Viaud J, et al. An allosteric kinase inhibitor binds the p21-activated kinase autoregulatory domain covalently. Mol Cancer Ther. 2009 Sep;8(9):2559-65.
[2]. Flaiz C, et al. PAK kinase regulates Rac GTPase and is a potential target in human schwannomas. Exp Neurol. 2009 Jul;218(1):137-44.
[3]. Deacon SW, et al.
溶解度数据
In Vitro: DMSO : 41.67 mg/mL (118.90 mM; ultrasonic and warming and heat to 60°C)配制储备液
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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