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Technical Data
| Formula | C20H14O2S2 |
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| Molecular Weight | 350.45 | CAS No. | 42521-82-4 | |
| Solubility (25°C)* | In vitro | DMSO | 70 mg/mL (199.74 mM) | |
| Ethanol | 7 mg/mL (19.97 mM) | |||
| Water | Insoluble | |||
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* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | 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). | ||
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| Targets |
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| 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] | ||
| Features | IPA-3 binds covalently to the Pak1 regulatory domain and prevents binding to the upstream activator Cdc42. |
Protocol (from reference)
References
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Customer Product Validation
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Data from [Data independently produced by , , Cell Death Differ, 2016, 23(1):169-81]
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Data from [Data independently produced by , , FASEB J, 2018, 32(1):73-82]
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Data from [Data independently produced by , , Fish Shellfish Immunol, 2019, 84:138-147]
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Data from [Data independently produced by , , Anticancer Res, 2017, 37(4):1805-1818]
Selleck's IPA-3 has been cited by 48 publications
| 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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.