IPA-3

SKU: orb1300672

Description

IPA-3

Research Area

Signal Transduction

Key Properties

• CAS Number: 42521-82-4
• MW: 350.45
• Purity: 97.40%
• Formula: C₂₀H₁₄O₂S₂
• SMILES: Oc1ccc2ccccc2c1SSc1c(O)ccc2ccccc12
• Target: PAK
• Solubility: DMSO:250 mg/mL (713.37 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.71 mM);Ethanol:7 mg/mL (19.97 mM)

Bioactivity

• Target IC50:
  PAK1:2.5 μM
• In Vitro:
  IPA-3 is a non-ATP-competitive, allosteric inhibitor of p21-activated kinase 1 (Pak1), with PIR3.5 serving as its control compound. It effectively blocks Cdc42-stimulated and sphingosine-dependent autophosphorylation of Pak1 on Thr423, without targeting the protein's exposed cysteine residues. The efficacy of IPA-3 is dependent on its disulfide bond; reduction by dithiothreitol (DTT) nullifies its inhibitory action on Pak1. Notably, IPA-3 obstructs Pak1 activation by various activators but does not affect already preactivated Pak1; it also impedes PDGF-induced Pak activation in mouse embryonic fibroblasts. This inhibition is partially achieved through covalent binding to Pak1's regulatory domain, an interaction that is both time- and temperature-sensitive, and prevents Cdc42 engagement. Additionally, IPA-3 demonstrates a direct bond to the Pak1 autoregulatory domain and offers reversible inhibition of PMA-induced membrane ruffling in cells.
• Cell Research:
  Human primary schwannoma cells are grown on 96 well plates for 2 days. Cells are left untreated or treated with 5 μM IPA-3, 20 μM IPA-3 or 20 μM PIR-3.5 for 24 hours. The MTS-solution is left on the cells for 3 hours, before the absorbance at 490 nm is measured. The experiments are conducted three times and mean and standard error of the mean is calculated with Excel.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, p21 activated kinases, PAK, PAK1, inhibit, IPA 3, IPA3, IPA-3

Compound Identifiers

PubChem CID

521106