IPA 3
Biological Activity
Group I p21-activated kinase (PAK) inhibitor (IC50 = 2.5 μM at PAK1). Targets the autoregulatory mechanism and promotes the inactive conformation of PAKs. Inhibits PAK1-mediated signaling in vivo; potential anti-tumor agent. Negative control PIR 3.5 (Cat. No. 4212) available.
Compound Libraries
IPA 3 is also offered as part of the Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 350.45 |
| Formula | C20H14O2S2 |
| Storage | Store at +4°C |
| Purity | ≥96% (HPLC) |
| CAS Number | 42521-82-4 |
| PubChem ID | 521106 |
| InChI Key | RFAXLXKIAKIUDT-UHFFFAOYSA-N |
| Smiles | OC2=C(SSC3=C(O)C=CC4=C3C=CC=C4)C1=CC=CC=C1C=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 26.28 | 75 | |
| ethanol | 3.5 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 350.45. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.85 mL | 14.27 mL | 28.53 mL |
| 5 mM | 0.57 mL | 2.85 mL | 5.71 mL |
| 10 mM | 0.29 mL | 1.43 mL | 2.85 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.57 mL |
Molarity Calculator
Reconstitution Calculator
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Kumar et al (2006) p21-activated kinases in cancer. Nat.Rev.Cancer 6 459 PMID: 16723992
Deacon et al (2008) An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase. Chem.Biol. 15 322 PMID: 18420139
Takahashi and Suzuki (2009) Membrane transport of WAVE2 and lamellipodia formation require Pak1 that mediates phosphorylation and recruitment of stathmin/op18 to Pak1-WAVE2-kinesin complex. Cell.Signal. 21 695 PMID: 19162178
Viaud and Peterson (2009) An allosteric kinase inhibitor binds the p21-activated kinase (Pak) autoregulatory domain covalently. Mol.Cancer Ther. 8 2559 PMID: 19723886
Wang et al (2016) P21-activated kinase inhibitors FRAX486 and IPA3: inhibition of prostate stromal cell growth and effects on smooth muscle contraction in the human prostate. PLoS One 11 e0153312 PMID: 27071060
If you know of a relevant reference for IPA 3, please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: Group I p21-activated kinases PAK PAK1 inhibitors inhibits IPA3 P21-activated Kinases
15 Citations for IPA 3
Citations are publications that use Tocris products. Selected citations for IPA 3 include:
Wu et al (2010) Pak1 and Pak2 are activated in recurrent respiratory papillomas, contributing to one pathway of Rac1-mediated COX-2 expression. Int J Cancer 127 2230 PMID: 20131316
Wang et al (2016) P21-activated kinase inhibitors FRAX486 and IPA3: inhibition of prostate stromal cell growth and effects on smooth muscle contraction in the human prostate. PLoS One 11 e0153312 PMID: 27071060
Salker et al (2016) LeftyA decreases Actin Polymerization and Stiffness in Human Endometrial Cancer Cells Scientific Reports 6 29370 PMID: 27404958
Imle et al (2015) Association with PAK2 Enables Functional Interactions of Lentiviral Nef Proteins with the Exocyst Complex. MBio 6 PMID: 26350970
Reinardy et al (2015) Phosphorylation of Threonine 794 on Tie1 by Rac1/PAK1 Reveals a Novel Angiogenesis Regulatory Pathway. PLoS One 10 e0139614 PMID: 26436659
Mortazavi et al (2015) Significance of KRAS/PAK1/Crk pathway in non-small cell lung cancer oncogenesis. BMC Cancer 15 381 PMID: 25956913
Oladimeji et al (2015) A Derivative of Differentiation-Inducing Factor-3 Inhibits PAK1 Activity and Breast Cancer Cell Proliferation. Am J Physiol Lung Cell Mol Physiol 2 42522 PMID: 26688830
Sorce et al (2015) Mitotic cells contract actomyosin cortex and generate pressure to round against or escape epithelial confinement. Oncotarget 6 8872 PMID: 26602832
Wang and Townes-Anderson (2015) LIM Kinase, a Newly Identified Regulator of Presynaptic Remodeling by Rod Photoreceptors After Injury. Nat Neurosci 56 7847 PMID: 26658506
Huttunen et al (2014) Coxsackievirus A9 infects cells via nonacidic multivesicular bodies. J Virol 88 5138 PMID: 24574401
Berger et al (2014) PAK-dependent STAT5 serine phosphorylation is required for BCR-ABL-induced leukemogenesis. Invest Ophthalmol Vis Sci 28 629 PMID: 24263804
Molosh et al (2014) Social learning and amygdala disruptions in Nf1 mice are rescued by blocking p21-activated kinase. Int J Cancer Clin Res 17 1583 PMID: 25242307
Al-Ejeh et al (2014) Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer. J Pharmacol Exp Ther 5 3145 PMID: 24762669
Martin et al (2013) Pak and Rac GTPases promote oncogenic KIT-induced neoplasms. J Clin Invest 123 4449 PMID: 24091327
Dipaolo et al (2013) Rac1 pathway mediates stretch response in pulmonary alveolar epithelial cells. Nat Commun 305 L141 PMID: 23686855
Do you know of a great paper that uses IPA 3 from Tocris? If so please let us know.
Literature in this Area
Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
Cardiovascular Research Product Guide
A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:
- Hypertension
- Thrombosis and Hemostasis
- Atherosclerosis
- Myocardial Infarction
- Ischemia/Reperfusion Injury
- Arrhythmias
- Heart Failure
Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
- Receptor Tyrosine Kinases
- Protein Kinases A, C, D and G
- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
- Receptor Serine/Threonine Kinases
