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Hedgehog/Smoothened Inhibitors | Agonists | Antagonists (11)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1082 Vismodegib (GDC-0449) Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.
  • Nature, 2014, 511(7507):90-3
  • Nat Med, 2014, 20(9):1035-42
  • Cancer Cell, 2014, 26(1):33-47
S1146 Cyclopamine Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.
  • Nature, 2015, 10.1038/nature14325
  • Cancer Res, 2012, 72(9):2262-74
  • Oncotarget, 2013, 4(10):1698-1711
S2151 LDE225 (NVP-LDE225,Erismodegib) 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) in cell-free assays, respectively. Phase 3.
  • Nat Chem Biol, 2013, 9(4):247-9
  • Br J Cancer, 2014, 111(6):1168-7
  • Mol Cancer, 2015, 10.1186/s12943-015-0345-x
S2157 Taladegib (LY2940680) Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.
S3042 Purmorphamine Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM.
S7779 Smoothened Agonist (SAG) HCl Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
S2777 PF-5274857 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.
S8075 GANT61 GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.
  • J Hepatol, 2014, 60(3):599-605
  • Br J Cancer, 2014, 111(6):1168-7
  • Mol Cell Biochem, 2014, 396(1-2):257-68
S7160 Glasdegib (PF-04449913) Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
S7092 SANT-1 SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.
S7138 BMS-833923 BMS-833923 is an orally bioavailable Smoothened antagonist. Phase 2.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1082 Vismodegib (GDC-0449) <1 mg/mL 84 mg/mL <1 mg/mL
S1146 Cyclopamine <1 mg/mL <1 mg/mL 2 mg/mL
S2151 LDE225 (NVP-LDE225,Erismodegib) <1 mg/mL 97 mg/mL 97 mg/mL
S2157 Taladegib (LY2940680) <1 mg/mL 0.66 mg/mL 2 mg/mL
S3042 Purmorphamine <1 mg/mL 4 mg/mL <1 mg/mL
S7779 Smoothened Agonist (SAG) HCl 100 mg/mL 71 mg/mL 40 mg/mL
S2777 PF-5274857 93 mg/mL 93 mg/mL <1 mg/mL
S8075 GANT61 <1 mg/mL <1 mg/mL 12 mg/mL
S7160 Glasdegib (PF-04449913) <1 mg/mL 47 mg/mL <1 mg/mL
S7092 SANT-1 <1 mg/mL 21 mg/mL 20 mg/mL
S7138 BMS-833923 <1 mg/mL 95 mg/mL <1 mg/mL
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