Smoothened Receptors

LDE225 (NVP-LDE225) is a potent, selective and orally bioavailable Smoothened (SMO) antagonist that inhibits hedgehog (Hh) signaling pathway via antagonism of the Smoothened receptor (SMO).

LY2940680 has been shown to affect a cancer cell signaling pathway initiated by the Hedgehog (Hh) protein.

LDE225 is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity.

PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ?? 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ?? 1.4 nmol/L in cells.

Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.

BMS-833923 (or XL-139) is an orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity.

SAG is a chlorobenzothiophene-containing compound which acts as a SMO agonist (EC50 = 3 nM) but inhibits hedgehog signaling at high concentrations (>1 uM).

PF-04449913 is a potent and orally bioavailable inhibitor of smoothened.

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

ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.

J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg/kg, respectively.

LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively.

MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.

SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM.

20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.