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Smo

Smoothened (Smo), a class Frizzled G protein-coupled receptor (class F GPCR), transduces the Hedgehog (Hh) signal across the cell membrane. The Hh signaling pathway includes both canonical and noncanonical pathways. The canonical Hh pathway functions through major Hh molecules such as Hh ligands, PTCH, Smo, and GLI, whereas the noncanonical Hh pathway involves the activation of Smo or GLI through other pathways. The Hh signaling cascade is initiated by the binding of the Hh protein ligand to its cellular membrane receptor, Patched (PTCH), which relieves PTCH-mediated repression of the seven-transmembrane (7TM) protein Smo. Activated Smo transduces the signal to the GLI family of transcription factors, which translocate to the nucleus to regulate numerous gene products involved in tissue patterning and cell differentiation.

Purmorphamine
T1810483367-10-8
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.
  • $35
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SAG
T1779912545-86-9
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.
  • $41
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Sonidegib
T1926956697-53-3
Sonidegib (Erismodegib), a Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.
  • $54
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Cyclopamine
T28254449-51-8
Cyclopamine (11-Deoxojervine), a Smoothened (Smo) antagonist (IC50: 46 nM in TM3Hh12 cells), belongs to the group of steroidal jerveratrum alkaloids.
  • $48
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SAG dihydrochloride
T404652702366-44-5
SAG dihydrochloride, a powerful agonist of the Smoothened (Smo) receptor (EC 50 = 3 nM; Kd = 59 nM), effectively activates the Hedgehog signaling pathway. It also negates the effects of Cyclopamine inhibition on Smo.
  • $59
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Jervine
T3363469-59-0
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.
  • $64
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SANT-1
T2450304909-07-7
SANT-1 directly binds to Smoothened (Smo) receptor (Kd: 1.2 nM) and inhibits Smo agonist effects (IC50: 20 nM).
  • $30
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20(S)-Hydroxycholesterol
T10085516-72-3In house
20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo).
  • $30
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Glasdegib
T65141095173-27-5
Glasdegib (PF-04449913) (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
  • $36
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SAG hydrochloride (912545-86-9(free base))
T42112095432-58-7
SAG hydrochloride (912545-86-9(free base)) (Smoothened Agonist HCl) acts as an SMO agonist.
  • $47
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LEQ506
T118381204975-42-7In house
LEQ506 is a Smo inhibitor with IC50s of 2 nM and 4 nM for hSmo and mSmo, respectively.
  • $58
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BMS-833923
T22991059734-66-5
BMS-833923 (XL-139), an orally bioavailable Smoothened antagonist, inhibits BODIPY cyclopamine binding to SMO in a dose-dependent manner (IC50: 21 nM).
  • $46
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ALLO-2
T141881357350-60-7
ALLO-2 is a Inhibitor of Drug-Resistant Smo Mutant.It inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.
  • $58
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Taladegib
T26661258861-20-9
Taladegib (LY2940680) is an orally bioavailable small molecule antagonist of the Hedgehog (Hh)-ligand cell surface receptor smoothened (Smo) with potential antineoplastic activity.
  • $35
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PF-5274857
T54651373615-35-0
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.
  • $30
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Saikosaponin B1
T391258558-08-0
Saponin activator. Activates release of Prostaglandin E2 in vitro. Anti-inflammatory agent. Orally active. Active in vivo and in vitro.
  • $57
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GSA-10
T22814300833-95-8
Smoothened (Smo) receptor agonist
  • $40
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CUR61414
T15019334998-36-6In house
CUR61414 is a cell-permeable inhibitor of Hedgehog signaling pathway (IC50 =100-200 nM) and selectively binds to smoothened (Ki = 44 nM).
  • $48
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MRT-83
T121091263131-92-5
MRT-83 is a potent Smo antagonist.
  • $38
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JNJ-1289
T60738792898-18-1
JNJ-1289 is a selective, potent, and competitive inhibitor of human spermine oxidase (hSMOX) with an IC50 value of 50 nM.JNJ-1289 has potential anticancer and anti-inflammatory activity for the study of polyamine catabolic disorders.
  • $83
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SMO-IN-2
T634291822355-27-0
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.
  • $111
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Sonidegib diphosphate
T157271218778-77-8
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).
  • $43
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Halcinonide
T01073093-35-4
Halcinonide (Halciderm), a high-efficiency corticosteroid, is served as an anti-inflammatory agent used in topical preparations.
  • $40
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HhAntag
T3460496794-70-8
HhAntag is a small molecule inhibitor of GLI1-mediated transcription, an essential down-stream element of the Hedgehog (Hh) pathway with the anti-tumor activity.
  • $44
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