Signaling Pathway

Smo

Smo

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Smoothened is a G protein-coupled receptor protein encoded by the SMO gene of the hedgehog signaling pathway conserved from flies to humans. It is the molecular target of the teratogen cyclopamine. Cellular localization plays an essential role in the function of SMO. Stimulation of the patched receptor by the sonic hedgehog ligand leads to translocation of SMO to the primary cilium. Furthermore, SMO that is mutated in the domain required for ciliary localisation cannot contribute to pathway activation.[3] SMO has also been shown to bind the kinesin motor protein Costal-2 and play a role in the localization of the Ci (Cubitus interruptus transcription factor) complex. SMO can function as an oncogene. Activating SMO mutations can lead to unregulated activation of the hedgehog pathway and cancer.

Smo Inhibitors & Modulators (12)

Product Name Catalog No. Brief Description
AMD 3465 hexahydrobromide

HY-15971

AMD 3465 6HBr(GENZ-644494) is a potent, selective CXCR4 antagonist; exhibits 8-fold higher affinity than AMD 3100; inhibits SDF-1α-ligand binding (Ki = 41.7 nM).

BMS-833923

HY-13809

BMS-833923 (XL-139) is an orally bioavailable small-molecule inhibitor of Smoothened  with potential antineoplastic activity;  inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner with an IC50 of 21 nM.

Halcinonide

HY-B0877

Halcinonide is a high potency corticosteroid used topically in the treatment of certain skin conditions.

Jervine

HY-N0836

Jervine(11-Ketocyclopamine) is a naturally occuring steroidal alkaloid that causes cyclopia by blocking sonic hedgehog(Shh) signaling; Jervine is an inhibitor of Smo.

LDE225

HY-16582A

LDE225 (NVP-LDE225; Erismodegib) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.

LDE225 Diphosphate

HY-16582

LDE225 Diphosphate (NVP-LDE225; Erismodegib) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.

LY2940680

HY-13242

LY2940680 binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling.

MK-4101

HY-100036

MK-4101 is a potent SMO Inhibitor of the Hedgehog Pathway, highly active against Medulloblastoma and Basal Cell Carcinoma.

PF-04449913

HY-16391

PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor.

PF-5274857

HY-13459

PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.

Purmorphamine

HY-15108

Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM and also is an inducer of osteoblast differentiation with EC50 of 1 μM.

SAG

HY-12848

SAG is a potent Smoothened (Smo) receptor agonist (Kd = 59 nM); potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM).