Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 39.00 | |
10 mg | In stock | $ 61.00 | |
25 mg | In stock | $ 118.00 | |
50 mg | In stock | $ 215.00 | |
100 mg | In stock | $ 379.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 43.00 |
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). |
Targets&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. |
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. |
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. |
Synonyms | IPA3, IPA 3 |
Molecular Weight | 350.45 |
Formula | C20H14O2S2 |
CAS No. | 42521-82-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 7 mg/mL (19.97 mM)
DMSO: 65 mg/mL (185.5 mM)
You can also refer to dose conversion for different animals. More
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IPA-3 42521-82-4 Cytoskeletal Signaling PAK inhibit Inhibitor IPA3 p21 activated kinases IPA 3 inhibitor