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IPA 3

Catalog #: 3622
32 Citations Datasheet
Catalog # Availability Size / Price Qty
3622/10
3622/50
IPA 3 | CAS No. 42521-82-4 | PAK Inhibitors
1 Image
Description: Group I PAK inhibitor

Chemical Name: 1,1'-Dithiodi-2-naphthtol

Purity: ≥96%

Product Details
Citations (32)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

IPA 3 is a 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.

Technical Data

M.Wt:
350.45
Formula:
C20H14O2S2
Solubility:
Soluble to 75 mM in DMSO
Purity:
≥96%
Storage:
Store at -20°C
CAS No:
42521-82-4

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.

Additional Information

Other Product-Specific Information:

Background References

  1. P21-Activated Kinase Inhibitors FRAX486 and IPA3: Inhibition of Prostate Stromal Cell Growth and Effects on Smooth Muscle Contraction in the Human Prostate.
    Wang Y, Gratzke C, Tamalunas A et al.
    PLoS One
  2. The bipartite rac1 Guanine nucleotide exchange factor engulfment and cell motility 1/dedicator of cytokinesis 180 (elmo1/dock180) protects endothelial cells from apoptosis in blood vessel development.
    Schaker K, Bartsch S, Patry C, Stoll S, Hillebrands J, Wieland T, Kroll J
    J Biol Chem, 2015;290(10):6408-18.
  3. PAK1 is a therapeutic target in acute myeloid leukemia and myelodysplastic syndrome.
    Pandolfi A, Stanley R, Yu Y, Bartholdy B, Pendurti G, Gritsman K, Boultwood J, Chernoff J, Verma A, Steidl U
    Blood, 2015;126(9):1118-27.
  4. Protein kinase D1 (PKD1) phosphorylation on Ser(203) by type I p21-activated kinase (PAK) regulates PKD1 localization
    JK Chang, Y Ni, L Han, J Sinnett-Sm, R Jacamo, O Rey, SH Young, E Rozengurt
    J. Biol. Chem., 2017;0(0):.
  5. LeftyA decreases Actin Polymerization and Stiffness in Human Endometrial Cancer Cells

    Sci Rep, 2016;6(0):29370.
  6. P21-Activated Kinase Inhibitors FRAX486 and IPA3: Inhibition of Prostate Stromal Cell Growth and Effects on Smooth Muscle Contraction in the Human Prostate
    Y Wang, C Gratzke, A Tamalunas, N Wiemer, A Ciotkowska, B Rutz, R Waidelich, F Strittmatt, C Liu, CG Stief, M Hennenberg
    PLoS ONE, 2016;11(4):e0153312.
  7. RhoJ Regulates Melanoma Chemoresistance by Suppressing Pathways That Sense DNA Damage.
    Ho H, Aruri J, Kapadia R, Mehr H, White M, Ganesan A
    Cancer Res, 2012;72(21):5516-28.
  8. p21-activated kinases in cancer.
    Kumar et al.
    Nat.Rev.Cancer, 2006;6:459
  9. An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase.
    Deacon et al.
    Chem.Biol., 2008;15:322
  10. Membrane transport of WAVE2 and lamellipodia formation require Pak1 that mediates phosphorylation and recruitment of stathmin/op18 to Pak1-WAVE2-kinesin complex.
    Takahashi and Suzuki
    Cell.Signal., 2009;21:695
  11. An allosteric kinase inhibitor binds the p21-activated kinase (Pak) autoregulatory domain covalently.
    Viaud and Peterson
    Mol.Cancer Ther., 2009;8:2559

Product Datasheets

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Citations for IPA 3

The citations listed below are publications that use Tocris products. Selected citations for IPA 3 include:

32 Citations: Showing 1 - 10

  1. Kinases of the Focal Adhesion Complex Contribute to Cardiomyocyte Specification.
    Authors: Brenda M Et al.
    Int J Mol Sci  2021;22
  2. Group I p21-activated kinases in leukemia cell adhesion to fibronectin.
    Authors: Petra Et al.
    Cell Adh Migr  2021;15:18-36
  3. Activation of Rac1 Has an Opposing Effect on Induction and Maintenance of Long-Term Potentiation in Hippocampus by Acting on Different Kinases.
    Authors: Li Et al.
    Front Mol Neurosci  2021;14:720371
  4. CtBP1-Mediated Membrane Fission Contributes to Effective Recycling of Synaptic Vesicles.
    Authors: Eckart D Et al.
    Cell Rep  2020;30:2444-2459.e7
  5. Interrogation of kinase genetic interactions provides a global view of PAK1-mediated signal transduction pathways.
    Authors: Marc Et al.
    J Biol Chem  2020;295:16906-16919
  6. Interrogation of kinase genetic interactions provides a global view of PAK1-mediated signal transduction pathways.
    Authors: Marc Et al.
    J Biol Chem  2020;295:16906-16919
  7. Sterically stabilized liposomes targeting P21 (RAC1) activated kinase-1 and secreted phospholipase A2 suppress prostate cancer growth and metastasis.
    Authors: Payaningal R Et al.
    Oncol Lett  2020;20:179
  8. PAK1 inhibitor IPA-3 mitigates metastatic prostate cancer-induced bone remodeling.
    Authors: Payaningal R Et al.
    Biochem Pharmacol  2020;177:113943
  9. Macropinocytosis drives T cell growth by sustaining the activation of mTORC1.
    Authors: Di Et al.
    Nat Commun  2020;11:180
  10. PAK Kinase Inhibition Has Therapeutic Activity in Novel Preclinical Models of Adult T-Cell Leukemia/Lymphoma.
    Authors: Amit Et al.
    Clin Cancer Res  2019;25:3589-3601
  11. Long-Term In Vitro Expansion of Epithelial Stem Cells Enabled by Pharmacological Inhibition of PAK1-ROCK-Myosin II and TGF-β Signaling.
    Authors: Zhang Et al.
    Cell Rep  2018;25:598
  12. Affecting long-term fear memory formation through optical control of Rac1 GTPase and PAK activity in lateral amygdala.
    Authors: Das Et al.
    Sci Rep  2017;7:13930
  13. RhoD Inhibits RhoC-ROCK-Dependent Cell Contraction via PAK6.
    Authors: Durkin Et al.
    Dev Cell  2017;41:315
  14. PAK proteins and YAP-1 signalling downstream of integrin beta-1 in myofibroblasts promote liver fibrosis.
    Authors: Martin Et al.
    Nat Commun  2016;7:12502
  15. LeftyA decreases Actin Polymerization and Stiffness in Human Endometrial Cancer Cells
    Authors: Salker Et al.
    Scientific Reports  2016;6:29370
  16. 1α,25(OH)2D3 Induces Actin Depolymerization in Endometrial Carcinoma Cells by Targeting RAC1 and PAK1.
    Authors: Zeng Et al.
    Cell Physiol Biochem  2016;40:1455
  17. P21-activated kinase inhibitors FRAX486 and IPA3: inhibition of prostate stromal cell growth and effects on smooth muscle contraction in the human prostate.
    Authors: Wang Et al.
    PLoS One  2016;11:e0153312
  18. Mitotic cells contract actomyosin cortex and generate pressure to round against or escape epithelial confinement.
    Authors: Sorce Et al.
    Oncotarget  2015;6:8872
  19. Association with PAK2 Enables Functional Interactions of Lentiviral Nef Proteins with the Exocyst Complex.
    Authors: Imle Et al.
    MBio  2015;6
  20. LIM Kinase, a Newly Identified Regulator of Presynaptic Remodeling by Rod Photoreceptors After Injury.
    Authors: Wang and Townes-Anderson
    Nat Neurosci  2015;56:7847
  21. A Derivative of Differentiation-Inducing Factor-3 Inhibits PAK1 Activity and Breast Cancer Cell Proliferation.
    Authors: Oladimeji Et al.
    Am J Physiol Lung Cell Mol Physiol  2015;2:42522
  22. Significance of KRAS/PAK1/Crk pathway in non-small cell lung cancer oncogenesis.
    Authors: Mortazavi Et al.
    BMC Cancer  2015;15:381
  23. PAK1 is a therapeutic target in acute myeloid leukemia and myelodysplastic syndrome.
    Authors: Pandolfi Et al.
    Blood  2015;126:1118
  24. Phosphorylation of Threonine 794 on Tie1 by Rac1/PAK1 Reveals a Novel Angiogenesis Regulatory Pathway.
    Authors: Reinardy Et al.
    PLoS One  2015;10:e0139614
  25. Coxsackievirus A9 infects cells via nonacidic multivesicular bodies.
    Authors: Huttunen Et al.
    J Virol  2014;88:5138
  26. Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer.
    Authors: Al-Ejeh Et al.
    J Pharmacol Exp Ther  2014;5:3145
  27. PAK-dependent STAT5 serine phosphorylation is required for BCR-ABL-induced leukemogenesis.
    Authors: Berger Et al.
    Invest Ophthalmol Vis Sci  2014;28:629
  28. Social learning and amygdala disruptions in Nf1 mice are rescued by blocking p21-activated kinase.
    Authors: Molosh Et al.
    Int J Cancer Clin Res  2014;17:1583
  29. Rac1 pathway mediates stretch response in pulmonary alveolar epithelial cells.
    Authors: Dipaolo Et al.
    Nat Commun  2013;305:L141
  30. Biphasic regulation of myosin light chain phosphorylation by p21-activated kinase modulates intestinal smooth muscle contractility.
    Authors: Ji Et al.
    J Biol Chem  2013;288:1200-13
  31. Pak and Rac GTPases promote oncogenic KIT-induced neoplasms.
    Authors: Martin Et al.
    J Clin Invest  2013;123:4449
  32. Pak1 and Pak2 are activated in recurrent respiratory papillomas, contributing to one pathway of Rac1-mediated COX-2 expression.
    Authors: Wu Et al.
    Int J Cancer  2010;127:2230

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