IPA-3

Description

Description

IPA-3 is a selective non-ATP competitive Pak1 inhibitor with IC50 of 2.5 μM, no inhibition to group II PAKs (PAKs 4-6).

2.5 μM ^[1]

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]

IPA-3 binds covalently to the Pak1 regulatory domain and prevents binding to the upstream activator Cdc42.

IPA-3

Catalog No.S7093

IPA-3 is a selective non-ATP competitive Pak1 inhibitor with IC50 of 2.5 μM, no inhibition to group II PAKs (PAKs 4-6).

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5mg	USD 88	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 466	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

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.

Solubility (25°C) *	In vitro	DMSO	70 mg/mL (199 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	7 mg/mL (19 mM)
* <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.