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Hedgehog/Smoothened Inhibitors | Agonists | Antagonists (10)


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.
  • 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.
  • 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
  • Br J Cancer, 2014, 111(6):1168-7
  • Mol Pharmacol, 2014, 83(5):1020-9
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 and also is an inducer of osteoblast differentiation with EC50 of 1 μM.
S7160 Glasdegib (PF-04449913) Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
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, 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
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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