IPA-3
Catalog No.S7093
Molecular Weight(MW): 350.45
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).
4 Customer Reviews
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(e) Immunoblot analysis of p-ERM, p-Pak1 and Pak1 in Ishikawa cells treated with various doses of Pak1 inhibitor IPA-3 for 24 h. Actin serves as a loading control
Cell Death Differ, 2016, 23(1):169-81. IPA-3 purchased from Selleck.
Effect of the PAK1-specific inhibitor IPA-3 on the regulatory role of PTPN12-S19E on EGF-induced cell migration. ***P < 0.001 vs. control; ##P < 0.01 vs. PRPN12-WT.
FASEB J, 2018, 32(1):73-82. IPA-3 purchased from Selleck.
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Effect of endocytic pathway inhibitors on the uptake of 0.5 μm and 1 μm beads by IgM+ and IgM− cells in peripheral blood leukocytes (PBL). A. Endocytic rate of IgM+ cells and IgM− cells for 0.5 μm beads in the presence of inhibitors (CPZ, dynasore, M-β-CD, nystatin, IPA-3, and NSC23766). B. Endocytic rate of IgM+ cells and IgM− cells for 1 μm beads in the presence of inhibitors. Data are obtained from three independent experiments. *, P < 0.05; **, P < 0.01.
Fish Shellfish Immunol, 2019, 84:138-147. IPA-3 purchased from Selleck.
The cells were treated with 5 μM of the PAK1-specific inhibitor IPA-3 or 1 μM of the ROCK1/2-specific inhibitor RKI-1447 for 24 h. Total cell lysates were immunoblotted with antibodies against p110β, p110δ, p-PAK1, PAK1, ROCK1, ROCK2, p-LIMK1, LIMK1 or β-actin, which served as an internal control. The results are representative of three independent experiments.
Anticancer Res, 2017, 37(4):1805-1818. IPA-3 purchased from Selleck.
Purity & Quality Control
Choose Selective PAK Inhibitors
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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| Features | IPA-3 binds covalently to the Pak1 regulatory domain and prevents binding to the upstream activator Cdc42. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 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] |
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| Cell Data |
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Protocol
Solubility (25°C)
| In vitro | DMSO | 70 mg/mL (199.74 mM) |
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| Ethanol | 7 mg/mL (19.97 mM) | |
| Water | 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.
Chemical Information
| Molecular Weight | 350.45 |
|---|---|
| Formula | C20H14O2S2 |
| CAS No. | 42521-82-4 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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Molarity Calculator
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
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Frequently Asked Questions
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Question 1:
If this product is cell membrane permeable and would it be suitable for PAK1 inhibition on a pancreatic beta cell line?
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Answer:
Based on the reference, I think IPA-3 is able to penetrate the cell membrane, it's likely to inhibit PAK1 on a pancreatic beta cell line although there is no reference confirming it: Figure 3: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3963893/; http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4353635/
