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Description: Group I PAK inhibitor
Chemical Name: 1,1'-Dithiodi-2-naphthtol
Purity: ≥96% (HPLC)
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 also 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 26.28 | 75 | |
| ethanol | 3.5 | 10 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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.75 mM | 3.8 mL | 19.02 mL | 38.05 mL |
| 3.75 mM | 0.76 mL | 3.8 mL | 7.61 mL |
| 7.5 mM | 0.38 mL | 1.9 mL | 3.8 mL |
| 37.5 mM | 0.08 mL | 0.38 mL | 0.76 mL |
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References
References are publications that support the biological activity of the product.
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.
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Keywords: IPA 3, IPA 3 supplier, Group, I, p21-activated, kinases, PAK, PAK1, inhibitors, inhibits, IPA3, P21-activated, Kinases, 3622, Tocris Bioscience
21 Citations for IPA 3
Citations are publications that use Tocris products. Selected citations for IPA 3 include:
Pandolfi et al (2015) PAK1 is a therapeutic target in acute myeloid leukemia and myelodysplastic syndrome. Blood 126 1118 PMID: 26170031
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
Huttunen et al (2014) Coxsackievirus A9 infects cells via nonacidic multivesicular bodies. J Virol 88 5138 PMID: 24574401
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
Das et al (2017) Affecting long-term fear memory formation through optical control of Rac1 GTPase and PAK activity in lateral amygdala. Sci Rep 7 13930 PMID: 29066727
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
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
Dipaolo et al (2013) Rac1 pathway mediates stretch response in pulmonary alveolar epithelial cells. Nat Commun 305 L141 PMID: 23686855
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
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
Martin et al (2013) Pak and Rac GTPases promote oncogenic KIT-induced neoplasms. J Clin Invest 123 4449 PMID: 24091327
Salker et al (2016) LeftyA decreases Actin Polymerization and Stiffness in Human Endometrial Cancer Cells Scientific Reports 6 29370 PMID: 27404958
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
Zhang et al (2018) Long-Term In Vitro Expansion of Epithelial Stem Cells Enabled by Pharmacological Inhibition of PAK1-ROCK-Myosin II and TGF-β Signaling. Cell Rep 25 598 PMID: 30332641
Zeng et al (2016) 1α,25(OH)2D3 Induces Actin Depolymerization in Endometrial Carcinoma Cells by Targeting RAC1 and PAK1. Cell Physiol Biochem 40 1455 PMID: 27997893
Durkin et al (2017) RhoD Inhibits RhoC-ROCK-Dependent Cell Contraction via PAK6. Dev Cell 41 315 PMID: 28486133
Martin et al (2016) PAK proteins and YAP-1 signalling downstream of integrin beta-1 in myofibroblasts promote liver fibrosis. Nat Commun 7 12502 PMID: 27535340
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
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Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
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- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
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