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Submit ReviewIPA 3
说明： Group I PAK inhibitor
化学名： 1,1'-Dithiodi-2-naphthtol
纯度： ≥96% (HPLC)
生物活性 for IPA 3
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.
技术数据 for IPA 3
| 分子量 | 350.45 |
| 公式 | C20H14O2S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for IPA 3
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 26.28 | 75 |
制备储备液 for IPA 3
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for IPA 3
参考文献 for IPA 3
参考文献是支持产品生物活性的出版物。
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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关键词: IPA 3, IPA 3 supplier, Group, I, p21-activated, kinases, PAK, PAK1, inhibitors, inhibits, IPA3, P21-activated, Kinases, 3622, Tocris Bioscience
32 篇 IPA 3 的引用文献
引用文献是使用了 Tocris 产品的出版物。 IPA 3 的部分引用包括：
Ji et al (2013) Biphasic regulation of myosin light chain phosphorylation by p21-activated kinase modulates intestinal smooth muscle contractility. J Biol Chem 288 1200-13 PMID: 23161543
Payaningal R et al (2020) PAK1 inhibitor IPA-3 mitigates metastatic prostate cancer-induced bone remodeling. Biochem Pharmacol 177 113943 PMID: 32240651
Marc et al (2020) Interrogation of kinase genetic interactions provides a global view of PAK1-mediated signal transduction pathways. J Biol Chem 295 16906-16919 PMID: 33453946
Eckart D et al (2020) CtBP1-Mediated Membrane Fission Contributes to Effective Recycling of Synaptic Vesicles. Cell Rep 30 2444-2459.e7 PMID: 32075774
Di et al (2020) Macropinocytosis drives T cell growth by sustaining the activation of mTORC1. Nat Commun 11 180 PMID: 31924779
Payaningal R et al (2020) Sterically stabilized liposomes targeting P21 (RAC1) activated kinase-1 and secreted phospholipase A2 suppress prostate cancer growth and metastasis. Oncol Lett 20 179 PMID: 32934746
Marc et al (2020) Interrogation of kinase genetic interactions provides a global view of PAK1-mediated signal transduction pathways. J Biol Chem 295 16906-16919 PMID: 33060198
Amit et al (2019) PAK Kinase Inhibition Has Therapeutic Activity in Novel Preclinical Models of Adult T-Cell Leukemia/Lymphoma. Clin Cancer Res 25 3589-3601 PMID: 30862694
Salker et al (2016) LeftyA decreases Actin Polymerization and Stiffness in Human Endometrial Cancer Cells Scientific Reports 6 29370 PMID: 27404958
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
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
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
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 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
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
Li et al (2021) Activation of Rac1 Has an Opposing Effect on Induction and Maintenance of Long-Term Potentiation in Hippocampus by Acting on Different Kinases. Front Mol Neurosci 14 720371 PMID: 34531724
Brenda M et al (2021) Kinases of the Focal Adhesion Complex Contribute to Cardiomyocyte Specification. Int J Mol Sci 22 PMID: 34638793
Petra et al (2021) Group I p21-activated kinases in leukemia cell adhesion to fibronectin. Cell Adh Migr 15 18-36 PMID: 33464167
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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