Home GPCR & G Protein Hedgehog/Smoothened

Hedgehog/Smoothened Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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.
Oncology Reports, October 18, 2018, 437-446
Frontiers in Oncology, November 10, 2020, 563838
Scientific Reports, May 15, 2017, 1899
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S8075 GANT 61 (NSC 136476) GANT61 (NSC 136476) 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. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.
Nat Commun, 2025, 16(1):1267
Theranostics, 2025, 15(18):9819-9837
J Exp Clin Cancer Res, 2025, 44(1):22
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S2476 Itraconazole Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. This compound is a potent antagonist of the Hedgehog (Hh) signaling pathway. It also suppresses the growth of glioblastoma through induction of autophagy.
Cell Rep Med, 2025, S2666-3791(25)00272-1
Infect Drug Resist, 2025, 18:783-789
Toxicol Appl Pharmacol, 2025, 502:117404
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S8249 HPI-4 (Ciliobrevin A) HPI-4 (Ciliobrevin A, Hedgehog Pathway Inhibitor 4) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.
Frontiers in Pharmacology, March 26, 2019, 290
Cell Communication and Signaling, February 18, 2026, 198
International Journal of Molecular Sciences, December 08, 2022, 15573
S2157 Taladegib (LY2940680) Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling in Phase 1/2.
PLOS One, November 16, 2015, e0142124
Journal of Dental Research, 2022, 1517-1525
Sci Rep, 2022, 12(1):7
S7160 Glasdegib Glasdegib is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
Journal of Extracellular Vesicles, September 23, 2025, e70163
Frontiers in Cell and Developmental Biology, September 13, 2021, 662868
J Extracell Vesicles, 2025, 14(9):e70163
S9743 Ciliobrevin D Ciliobrevin D (compound 5) is a cell-permeable, reversible and specific antagonist of AAA+ (ATPases associated with diverse cellular activities) ATPase motor cytoplasmic dynein. This compound perturbs primary cilia formation and blocks Hedgehog (Hh) signaling.
Cell Prolif, 2025, e13819.
ACS Chem Biol, 2024, 19(8):1733-1742
Mol Cell, 2022, S1097-2765(22)00327-6
S4747 Jervine Jervine (11-Ketocyclopamine) is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened.
FASEB J, 2025, 39(20):e71187
Sci Rep, 2022, 12(1):7
Neurochem Int, 2021, 146:105042
S6565 JK184 JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells.
Cell Res, 2020, 10.1038/s41422-020-00426-0
Harvard University (Doctoral dissertation), 2016, nan
S8200 MK-4101 MK-4101, a potent inhibitor of the Hedgehog pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells.
Sci Rep, 2022, 12(1):7
E0782 MRT 10 MRT-10 inhibits ShhN signaling in Shh-light2 cells in a dose-dependent manner with IC50 of 0.64 μM, showing the capacity to abrogate the constitutive activity of Smo.