PP2 is a potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases. PP2 strongly inhibits the kinases Lck (IC50=4 nM), Fyn (5 nM) and Hck (5 nM). PP2 also inhibits anti-CD3-stimulated tyrosine phosphorylation of human T-cells with an IC50 value of 600 nM. PP2 does not significantly affect the activity of EGFR kinase (IC50 = 480 nM), JAK2 (IC50 > 50 µM), or ZAP-70 (IC50 > 100 µM).
Oncotarget. 2016 Feb 22.
|Source||Oncotarget (2016). Figure 11. Inhibitors of PI3K (LY294002), Akt (MK-2206), Src (PP2), FAK (PF573228) and mTOR (rapamycin) were purchased from Abmole Bioscience (Houston, TX, USA).|
|Cell Lines||MDA-MB-231 cells|
|Concentrations||PI3K (10 µM LY294002), Akt (10 µM MK-2206) or mTOR (10 µM rapamycin)|
|Results||As shown in Figure 11. Pretreating MDA-MB-231 cells with the specific inhibitors of PI3K (10 µM LY294002), Akt (10 µM MK-2206) and mTOR (10 µM rapamycin) completely abolished the LSS-induced MT1-MMP expression, indicating that the PI3K/Akt/mTOR pathway is required for LSS-induced MT1-MMP expression.|
|Source||Oncotarget (2016). Figure 1. Inhibitors of PI3K (LY294002), Akt (MK-2206), Src (PP2), FAK (PF573228) and mTOR (rapamycin) were purchased from Abmole Bioscience (Houston, TX, USA).|
|Method||Cell motility assay|
|Cell Lines||MDA-MB-231 cells|
|Concentrations||PI3K (10 μM LY294002), Akt (20 μM MK-2206), mTOR (10 μM rapamycin, Rap), FAK (10 μM PF573228) or Src (10 μM PP2)|
|Results||"Notably, inhibitors of PI3K (LY294002), Akt (MK-2206) and mTOR (rapamycin) markedly decreased the LSS-induced wound closure activity. However, pretreatment with inhibitors of FAK (PF573228) and Src (PP2) has no effect on the LSS-induced cell motility (Figure 1B). It is suggested that PI3K, Akt and mTOR might be participated LSS-induced cell motility in an FAK and Src-independent manner. "|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 20 mg/mL|
Src family kinase inhibitor PP2 efficiently inhibits cervical cancer cell proliferation through down-regulating phospho-Src-Y416 and phospho-EGFR-Y1173.
Kong L, et al. Mol Cell Biochem. 2011 Feb;348(1-2):11-9. PMID: 21052789.
Src family kinase inhibitor PP2 restores the E-cadherin/catenin cell adhesion system in human cancer cells and reduces cancer metastasis.
Nam JS, et al. Clin Cancer Res. 2002 Jul;8(7):2430-6. PMID: 12114449.
Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation.
Hanke JH, et al. J Biol Chem. 1996 Jan 12;271(2):695-701. PMID: 8557675.
|Related Src-bcr-Abl Products|
TG-100572 hydrochloride is a potent and selective multi-targeted VEGFR2/Src kinase inhibitor.
Ponatinib hydrochloride is a potent, orally available multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
AMG-47a is a potent inhibitor of Lck and T cell proliferation; exhibits anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.
GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.
Radotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.