Name: PP 2 (AG 1879)
Price: 206.00 USD

- Overview
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    Background
    
    PP2 is a selective inhibitor of Src family with IC50 value of 4 nM and 5 nM for Lck and Fyn, respectively [1].Src is a tyrosine kinase and contains 9 members: c-Src (this protein), Yes, Fyn, Fgr, Yrk, Lyn, Blk, Hck, and Lck [1].PP2 is a potent Src family inhibitor that plays an important role in the cancer and is regarded as a promising target for treatment. When tested with human glioma cell line U251 spheroids in 3-D model, PP2 inhibited the cell invasion in a dose-dependent manner (2.5 μM, 10μM). And treated monolayer U251 cells with PP2 (10μM) decreased cell proliferation rate by inhibiting Src [2]. In human T cells, PP2 showed inhibition on anti-CD3-induced tyrosine phosphorylation by inhibiting Lck and Fyn that involved in the early T cell signal transduction [1].In Sprague-Dawley rat model injected with urethane and after some needed treatment to perform research and record data, pretreatment with PP2 (50M, 10μL it) reversed the reflex potentiation, as well as Src kinase and NR2B phosphorylation by inhibiting Src family [3].It is also reported that PP2 inhibits ZAP-70, JAK2 and EGF-R with IC50 value of >100 μM, >50 μM, and 480 nM, respectively [1].
    
    [1]. Hanke, J.H., et al., Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. J Biol Chem, 1996. 271(2): p. 695-701.
    [2]. Angers-Loustau, A., et al., SRC regulates actin dynamics and invasion of malignant glial cells in three dimensions. Mol Cancer Res, 2004. 2(11): p. 595-605.
    [3]. Wu, H.C., et al., EphrinB2 induces pelvic-urethra reflex potentiation via Src kinase-dependent tyrosine phosphorylation of NR2B. Am J Physiol Renal Physiol, 2011. 300(2): p. F403-11.
- Properties
  - Alternative Name
    
    1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-amine
    
    CAS Number
    
    172889-27-9
    
    Molecular Formula
    
    C15H16ClN5
    
    Molecular Weight
    
    301.78
    
    Appearance
    
    A solid
    
    Purity
    
    99.39%
    
    Solubility
    
    insoluble in H2O; ≥15.1 mg/mL in DMSO; ≥20.05 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Desiccate at 4°C
    
    * For Research Use Only
- Reference
  - 1. Zhang XH, Li CY, et al. "Pro-angiogenic activity of isoliquiritin on HUVECs in vitro and zebrafish in vivo through Raf/MEK signaling pathway." Life Sci. 2019 Apr 15;223:128-136. PMID:30876941

PP 2 (AG 1879)

PP 2 (AG 1879)

Background

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