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Hedgehog/Smoothened Inhibitors | Agonists | Antagonists (9)


Cat.No. Product Name Information Product Citations Customer Reviews
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.
  • Nature, 2014, 10.1038/nature13283
  • Gastroenterology, 2012, 143(5):1319-29.e1-11
  • Gut, 2012, 61(9):1323-9
S1146 Cyclopamine Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM.
  • Cancer Res, 2012, 72(9):2262-74
  • Oncotarget, 2013, 4(10):1698-1711
  • Neuro Oncol, 2012, 14(12):1441-51
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), respectively. Phase 3.
  • Nat Chem Biol, 2013, 9(4):247-9
  • Mol Pharmacol, 2014, 83(5):1020-9
S2157 LY2940680 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 and also is an inducer of osteoblast differentiation with EC50 of 1 μM.
S7138 BMS-833923 BMS-833923 is an orally bioavailable Smoothened antagonist. Phase 2.
S8075 GANT61 GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.
  • J Hepatol, 2014, 60(3):599-605
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.
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.