Chemical Name: 1,1'-Dithiodi-2-naphthtol
Biological ActivityGroup 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.
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.
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.
p21-activated kinases in cancer.
Kumar et al.
An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase.
Deacon et al.
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
An allosteric kinase inhibitor binds the p21-activated kinase (Pak) autoregulatory domain covalently.
Viaud and Peterson
Mol.Cancer Ther., 2009;8:2559
Citations for IPA 3
The citations listed below are publications that use Tocris products. Selected citations for IPA 3 include:
21 Citations: Showing 1 - 10
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
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
RhoD Inhibits RhoC-ROCK-Dependent Cell Contraction via PAK6.
Authors: Durkin Et al.
Dev Cell 2017;41:315
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
LeftyA decreases Actin Polymerization and Stiffness in Human Endometrial Cancer Cells
Authors: Salker Et al.
Scientific Reports 2016;6:29370
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
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
Mitotic cells contract actomyosin cortex and generate pressure to round against or escape epithelial confinement.
Authors: Sorce Et al.
Association with PAK2 Enables Functional Interactions of Lentiviral Nef Proteins with the Exocyst Complex.
Authors: Imle Et al.
LIM Kinase, a Newly Identified Regulator of Presynaptic Remodeling by Rod Photoreceptors After Injury.
Authors: Wang and Townes-Anderson
Nat Neurosci 2015;56:7847
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
Significance of KRAS/PAK1/Crk pathway in non-small cell lung cancer oncogenesis.
Authors: Mortazavi Et al.
BMC Cancer 2015;15:381
PAK1 is a therapeutic target in acute myeloid leukemia and myelodysplastic syndrome.
Authors: Pandolfi Et al.
Phosphorylation of Threonine 794 on Tie1 by Rac1/PAK1 Reveals a Novel Angiogenesis Regulatory Pathway.
Authors: Reinardy Et al.
PLoS One 2015;10:e0139614
Coxsackievirus A9 infects cells via nonacidic multivesicular bodies.
Authors: Huttunen Et al.
J Virol 2014;88:5138
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
PAK-dependent STAT5 serine phosphorylation is required for BCR-ABL-induced leukemogenesis.
Authors: Berger Et al.
Invest Ophthalmol Vis Sci 2014;28:629
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
Rac1 pathway mediates stretch response in pulmonary alveolar epithelial cells.
Authors: Dipaolo Et al.
Nat Commun 2013;305:L141
Pak and Rac GTPases promote oncogenic KIT-induced neoplasms.
Authors: Martin Et al.
J Clin Invest 2013;123:4449
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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