Smo

LEQ506 is a Smo inhibitor with IC50s of 2 nM and 4 nM for hSmo and mSmo, respectively.

Halcinonide (Halciderm), a high-efficiency corticosteroid, is served as an anti-inflammatory agent used in topical preparations.

GI-560192 (RL-0070933) is a potent smo cilial modulator with an EC50 value of 0.02 µM. GI-560192 modulates the translocation and/or accumulation of smoothened to the primary cilia by hedgehog signaling pathway.

MRT-14 is a potent Smo antagonist and can be used in several types of cancers linked to abnormal Hh signaling studies.

MRT-83 is a potent Smo antagonist.

Sonidegib diphosphate (LDE225 diphosphate) is a selective antagonist of Smo that inhibits murine Smo (IC50:1.3 nM) and human Smo (IC50:2.5 nM).

Saridegib is an effective and specific inhibitor of Smoothened and a key signaling transmembrane protein in the Hedgehog pathway.

SAG (Smoothened Agonist) is a Smo receptor agonist (EC50=3 nM) that is cell-permeable and selective. SAG regulates Smo activity by binding directly to the Smo helix and can activate the Hedgehog signaling pathway.

Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo. It also is an inducer of osteoblast differentiation.

Sonidegib (Erismodegib), a Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.

SANT-1 directly binds to Smoothened (Smo) receptor (Kd: 1.2 nM) and inhibits Smo agonist effects (IC50: 20 nM).

Taladegib (LY2940680) is an orally bioavailable small molecule antagonist of the Hedgehog (Hh)-ligand cell surface receptor smoothened (Smo) with potential antineoplastic activity.

AZD8542 is an antagonist of Smoothened (SMO) with potential as an [oncology therapeutic].

Cyclopamine (11-Deoxojervine), a Smoothened (Smo) antagonist (IC50: 46 nM in TM3Hh12 cells), belongs to the group of steroidal jerveratrum alkaloids.

The biological activity of Jervine (Jerwiny) is mediated via its interaction with the 7 passes transmembrane protein Smoothened. Jervine binds with and inhibits smoothened, which is an integral part of the Hedgehog signaling pathways. With smoothened inhibited, the GLI1 transcription cannot be activated and Hedgehog target genes cannot be transcribed.

PF-5274857 (PF-5274857 free base) is an effective and selective hedgehog signaling pathway inhibitor (IC50: 5.8 nM and a Ki: 4.6 nM). PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.PF-5274857 was found to effectively penetrate the blood-brain barrier and inhibit Smo activity in the brain of primary medulloblastoma mice, resulting in improved animal survival rates. PF-5274857 was orally available and metabolically stable in vivo.

Glasdegib (PF-04449913) (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.

MK-4101, an effective inhibitor of the Hedgehog pathway, has anti-tumor activity through the induction of extensive apoptosis and inhibition of proliferation in tumor cells.

MRT-81 is a potent antagonist of human and rodent smoothened receptors that inhibits hedgehog activity with an IC50 value of 41 nM in Shh-light2 cells.It is used in the study of cancer.

SMO-IN-1 (Compound 15) is an orally effective Smoothened (SMO) inhibitor with an EC50 value of 89 nM for sonic Hh protein (shh).

SMO-IN-3 is a potent inhibitor of smoothened (SMO) that acts on the hedgehog (Hh) signaling pathway (IC50: 34.09 nM). SMO-IN-3 inhibits the proliferation of Daoy, a human medulloblastoma cell line, and exhibits anticancer effects.

SMO-IN-2 is a potent smoothened (SMO) inhibitor of hedgehog (Hh) signaling.SMO-IN-2 shows antiproliferative activity and anticancer activity against human medulloblastoma cell lines.SMO-IN-2 can be used in the study of cancer.

SMO-IN-5 (Compound 25(B31)) is an effective inhibitor of smoothened (SMO), which suppresses the Hedgehog (Hh) signaling pathway. This compound inhibits cellular proliferation and induces apoptosis, demonstrating antitumor activity.

20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo).