IPA-3

製品コードS7093 バッチS709301

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H14O2S2
分子量 350.45 CAS No. 42521-82-4
Solubility (25°C)* 体外 DMSO 70 mg/mL (199.74 mM)
Ethanol 7 mg/mL (19.97 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 IPA-3 is a selective non-ATP competitive Pak1 inhibitor with IC50 of 2.5 μM in a cell-free assay, no inhibition to group II PAKs (PAKs 4-6).
in vitro 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. [1] 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. [2]
特徴 IPA-3 binds covalently to the Pak1 regulatory domain and prevents binding to the upstream activator Cdc42.

プロトコル(参考用のみ)

キナーゼアッセイ Kinase assay
Pak1 (150 nM final) is pre-incubated with MBP (8.3 μM), indicated proteins, and IPA-3 or DMSO in Kinase buffer for 20 minutes at 4°C. Cdc42-GTPγS (3.2 μM) is then added and the reaction is pre-equilibrated 10 minutes at 30 °C. Kinase reactions are started by the addition of ATP (to 30 μM) containing [32P]ATP and are incubated 10 min and analyzed by SDS-PAGE and autoradiography.

カスタマーフィードバック

Data from [Data independently produced by , , Cell Death Differ, 2016, 23(1):169-81]

Data from [Data independently produced by , , FASEB J, 2018, 32(1):73-82]

Data from [Data independently produced by , , Fish Shellfish Immunol, 2019, 84:138-147]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

PAK1-Dependent Regulation of Microtubule Organization and Spindle Migration Is Essential for the Metaphase I-Metaphase II Transition in Porcine Oocytes [ Biomolecules, 2024, 14(2)237] PubMed: 38397472
A GSTP1-mediated lactic acid signaling promotes tumorigenesis through the PPP oxidative branch [ Cell Death Dis, 2023, 14(7):463] PubMed: 37491277
A GSTP1-mediated lactic acid signaling promotes tumorigenesis through the PPP oxidative branch [ Cell Death Dis, 2023, 14(7):463] PubMed: 37491277
PAK1 contributes to cerebral ischemia/reperfusion injury by regulating the blood-brain barrier integrity [ iScience, 2023, 26(8):107333] PubMed: 37529106
PAK1 Is Involved in the Spindle Assembly during the First Meiotic Division in Porcine Oocytes [ Int J Mol Sci, 2023, 24(2)1123] PubMed: 36674642
High extracellular glucose promotes cell motility by modulating cell deformability and contractility via the cAMP-RhoA-ROCK axis in human breast cancer cells [ Mol Biol Cell, 2023, 34(8):ar79] PubMed: 37195739
Activation of CD44/PAK1/AKT signaling promotes resistance to FGFR1 inhibition in squamous-cell lung cancer [ NPJ Precis Oncol, 2022, 6(1):52] PubMed: 35853934
Delivery of Basic Fibroblast Growth Factor Through an In Situ Forming Smart Hydrogel Activates Autophagy in Schwann Cells and Improves Facial Nerves Generation via the PAK-1 Signaling Pathway [ Front Pharmacol, 2022, 13:778680] PubMed: 35431972
Channel catfish virus entry into host cells via clathrin-mediated endocytosis [ Virus Res, 2022, 315:198794] PubMed: 35504448
The Smad4-MYO18A-PP1A complex regulates β-catenin phosphorylation and pemigatinib resistance by inhibiting PAK1 in cholangiocarcinoma [ Cell Death Differ, 2021, 10.1038/s41418-021-00897-7] PubMed: 34799729

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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