LY2940680 is a selective inhibitor of Smo receptor and thus inhibits Hh signaling pathway .
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 .
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 . 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 .
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 .
. 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.
. 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.
. Redmond, E.M., et al., Investigational Notch and Hedgehog inhibitors--therapies for cardiovascular disease. Expert Opin Investig Drugs, 2011. 20(12): p. 1649-64.
|Physical Appearance||A crystalline solid|
|Storage||Store at -20°C|
|Solubility||≥51.3mg/mL in DMSO with ultrasonic and warming|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Description||LY2940680 is a potent inhibitor of Smoothened (Smo) receptor and Hedgehog (Hh) signaling.|