IPA-3

製品コードS7093 バッチS709301

化学情報

	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は、無細胞アッセイにおいてIC50が2.5 μMの選択的非ATP競合的Pak1阻害剤であり、グループII PAKs（PAKs 4-6）に対する阻害作用はありません。
in vitro	IPA-3 is a non ATP-competitive, allosteric inhibitor of p21-activated kinase 1 (Pak1). PIR3.5 is the control compound of this compound. It prevents Cdc42-stimulated Pak1 autophosphorylation on Thr423. This compound also prevents sphingosine-dependent Pak1 autophosphorylation. It does not target exposed cysteine residues on Pak1. The disulfide bond of this inhibitor is critical for inhibition of Pak1 and in vitro reduction by the reducing agent dithiothreitol (DTT) abolishes Pak1 inhibition by this chemical. It inhibits activation of Pak1 by diverse activators, but does not inhibit preactivated Pak1. This compound inhibits PDGF-stimulated Pak activation in mouse embryonic fibroblasts. It inhibits Pak1 activation in part by binding covalently to the regulatory domain of Pak1. This chemical binds Pak1 covalently in a time- and temperature-dependent manner. It prevents binding of the Pak1 activator Cdc42. This inhibitor binds directly to the Pak1 autoregulatory domain. It reversibly inhibits PMA-induced membrane ruffling in cells.
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
キナーゼアッセイ	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.

参考

https://pubmed.ncbi.nlm.nih.gov/18420139/
https://pubmed.ncbi.nlm.nih.gov/19723886/

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：

A novel PAK1/TCF1 regulatory axis promotes non-small cell lung cancer progression [ Discov Oncol, 2025, 16(1):364]	PubMed: 40111665
Gadd45g insufficiency drives the pathogenesis of myeloproliferative neoplasms [ Nat Commun, 2024, 15(1):2989]	PubMed: 38582902
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
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

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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