IPA-3 NEW
| Price | $39 | $61 | $118 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: IPA-3 | CAS No.: 42521-82-4 |
| Purity: 90% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | IPA-3 |
| Description | IPA-3 is a selective, non-ATP competitive Pak1 inhibitor with an IC50 of 2.5 μM, and it does not inhibit group II PAKs (PAKs 4-6). |
| 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. |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 7 mg/mL (19.97 mM) DMSO : 65 mg/mL (185.5 mM) |
| Keywords | inhibit | Inhibitor | IPA-3 | p21 activated kinases | PAK |
| Inhibitors Related | Fingolimod hydrochloride | ZINC194100678 | PIR 3.5 | PF-3758309 hydrochloride | G-5555 | FRAX1036 | FRAX597 | NVS-PAK1-1 | GNE 2861 | 5-Aminosalicylic Acid | Fingolimod | FRAX486 HCL(1232030-35-1 free base) |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Featured Novel Bioactive Compound Library | Kinase Inhibitor Library | Inhibitor Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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