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Smoothened

Smoothened (smo), a G protein-coupled receptor, drives the Hedgehog signalling pathway and is involved in gene expression and Gli family transcription factors. The core members of the Smo signalling pathway include the ligand (Hedgehog, Hh), the receptor (Patched, Ptc), several transducers such as Smoothened (Smo) and the ytoplasmic complex formed by the kinesin-like protein Costal-2 (Cos2), the serine/threonine kinase Fused (Fu), the novel protein Suppressor of fused [Su(fu)], and the transcription factor Cubitus interruptus (Ci). SMO is classified as a proto-oncogene because the tumour suppressor PTCH represses signalling by SMO, and SHH relieves this repression.

Inhibitors

Cat.No. Product Name Information Publication Customer Review
S2151 LDE225 (NVP-LDE225, Erismodegib) LDE225 (NVP-LDE225) is a smoothened antagonist with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively. (1)
S2157 LY2940680 LY2940680 binds to the Smo receptor and potently inhibits Hh signaling.
S2777 PF-5274857 PF-5274857 is a potent and selective Smoothened (Smo) antagonist with IC50 and Ki of 5.8 nM and 4.6 nM, respectively.

Smoothened

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