Name: LY2940680
Price: 381.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    LY2940680 is a selective inhibitor of Smo receptor and thus inhibits Hh signaling pathway [1].
    Smoothened(Smo) receptor is a member of class F G protein-coupled receptors, which plays an important role in the main transducer of the Hedgehog (Hh) signaling pathway that implicated in a wide range of developmental and adult processes [2].
    LY2940680 is a potent Smo receptor inhibitor that binds mostly to extracelluar loops and has a different functioning site with the reported Smo receptor inhibitor SANT-1 which binds to 7TM [2]. When tested with cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib, LY2940680 inhibited cell proliferation [3].
    Many studies have shown that Hh signaling pathway plays a pivotal role in CSCs and Hh inhibition caused many aspects of transformation attributed to CSCs. In patients with basal cell carcinoma and medulloblastoma, LY2940680 showed good efficacy as a monotherapy [1].
    
    [1]. Justilien, V. and A.P. Fields, Molecular pathways: novel approaches for improved therapeutic targeting of Hedgehog signaling in cancer stem cells. Clin Cancer Res, 2015. 21(3): p. 505-13.
    [2]. Hoch, L., et al., MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. Faseb j, 2015. 29(5): p. 1817-29.
    [3]. Redmond, E.M., et al., Investigational Notch and Hedgehog inhibitors--therapies for cardiovascular disease. Expert Opin Investig Drugs, 2011. 20(12): p. 1649-64.
- Properties
  - Alternative Name
    
    4-fluoro-N-methyl-N-[1-[4-(2-methylpyrazol-3-yl)phthalazin-1-yl]piperidin-4-yl]-2-(trifluoromethyl)benzamide
    
    CAS Number
    
    1258861-20-9
    
    Molecular Formula
    
    C26H24F4N6O
    
    Molecular Weight
    
    512.5
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥5.2 mg/mL in EtOH with ultrasonic; ≥51.3 mg/mL in DMSO with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

LY2940680

LY2940680

Background

We Also Recommend

HPI 1

JK 184

SANT-2