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Purity: ≥98%
IPA-3 (IPA3; IPA 3) is a novel, potent, selective and non-ATP competitive PAK1 (p21-activated protein kinase 1) inhibitor with potential antitumor activity. It inhibits the growth of liver cancer cells by suppressing PAK1 and NF-κB activation and has IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).
| ln Vitro |
Part of the mechanism by which IPA-3 suppresses Pak1 activation is covalent attachment to Pak1's regulatory domain. Pak1 is covalently bound by IPA-3 in a temperature- and time-dependent manner. Binding of the Pak1 activator Cdc42 is inhibited by IPA-3. Direct binding of IPA-3 occurs with the Pak1 autoregulatory domain. In cells, IPA-3 reversibly prevents PMA-induced membrane ruffling[1]. Human primary Schwann and schwannoma cells exhibit reduced cell spreading in response to IPA-3 (2 μM, 5 μM, or 20 μM). In a dose-dependent manner, IPA-3 therapy dramatically lowers adherent Schwann and schwannoma cell counts[2]. IPA-3 is an allosteric inhibitor of p21-activated kinase 1 (Pak1) that is non-ATP-competitive. The IPA-3 control chemical is PIR3.5. On Thr423, IPA-3 inhibits the autophosphorylation of Pak1 induced by Cdc42. Additionally, sphingosine-dependent Pak1 autophosphorylation is inhibited by IPA-3. IPA-3 does not specifically target Pak1's exposed cysteine residues. The disulfide bond in IPA-3 is essential for the inhibition of Pak1, and Pak1 inhibition by IPA-3 is eliminated in vitro when the reducing agent dithiothreitol (DTT) is reduced. IPA-3 prevents different activators from activating Pak1, but it has no effect on Pak1 that has already been activated. In mouse embryonic fibroblasts, IPA-3 suppresses the activation of Pak in response to PDGF[3].
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| References |
[1]. Viaud J, et al. An allosteric kinase inhibitor binds the p21-activated kinase autoregulatory domain covalently. Mol Cancer Ther. 2009 Sep;8(9):2559-65.
[2]. Flaiz C, et al. PAK kinase regulates Rac GTPase and is a potential target in human schwannomas. Exp Neurol. 2009 Jul;218(1):137-44. [3]. Deacon SW, et al. An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase. Chem Biol. 2008 Apr;15(4):322-31 |
| Molecular Formula |
C20H14O2S2
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| Molecular Weight |
350.45
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| CAS # |
42521-82-4
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| Related CAS # |
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| SMILES |
OC1=CC=C2C=CC=CC2=C1SSC3=C4C=CC=CC4=CC=C3O
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| InChi Key |
RFAXLXKIAKIUDT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H14O2S2/c21-17-11-9-13-5-1-3-7-15(13)19(17)23-24-20-16-8-4-2-6-14(16)10-12-18(20)22/h1-12,21-22H
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| Chemical Name |
1,1-disulfanediylbis(naphthalen-2-ol)
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8535 mL | 14.2674 mL | 28.5347 mL | |
| 5 mM | 0.5707 mL | 2.8535 mL | 5.7069 mL | |
| 10 mM | 0.2853 mL | 1.4267 mL | 2.8535 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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