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).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 9,000 | |||
10 mg | 在庫あり | ¥ 14,000 | |||
25 mg | 在庫あり | ¥ 27,000 | |||
50 mg | 在庫あり | ¥ 49,500 | |||
100 mg | 在庫あり | ¥ 87,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 10,000 |
ターゲット&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. |
別名 | IPA3, IPA 3 |
分子量 | 350.45 |
分子式 | 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. 詳細
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IPA-3 42521-82-4 Cytoskeletal Signaling PAK inhibit Inhibitor IPA3 p21 activated kinases IPA 3 inhibitor