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.
Nat Commun, 2025, 16(1):5137
Nat Commun, 2025, 16(1):1092
Nat Commun, 2025, 16(1):1267
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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.
Commun Biol, 2025, 8(1):607
International Journal of Molecular Sciences, 2025, 2138
Int J Mol Sci, 2025, 26(5)2138
S2157 Taladegib (LY2940680) Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling in Phase 1/2.
Sci Rep, 2022, 12(1):7
Carcinogenesis, 2020, 41(7):993-1004
Front Pharmacol, 2019, 10:89
S7160 Glasdegib Glasdegib is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
J Extracell Vesicles, 2025, 14(9):e70163
iScience, 2024, 27(10):110862
Leukemia, 2023, 37(8):1649-1659
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
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
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
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.