Hedgehog/Smoothened Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S7138	BMS-833923	BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.	Nat Commun, 2025, 16(1):4983 Sci Rep, 2022, 12(1):7 Mol Cancer Res, 2021, molcanres.MCR-21-0257-A.2021
S2157	Taladegib (LY2940680)	Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signalling 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 an 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) signalling.	Cell Prolif, 2025, e13819. ACS Chem Biol, 2024, 19(8):1733-1742 Mol Cell, 2022, S1097-2765(22)00327-6
S2777	PF-5274857	PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signalling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and this compound can penetrate the blood–brain barrier.	Sci Rep, 2022, 12(1):7 Biol Reprod, 2021, ioab111 Carcinogenesis, 2020, 41(7):993-1004
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-tumour activity through the inhibition of proliferation and induction of extensive apoptosis in tumour cells.	Sci Rep, 2022, 12(1):7
S6565	JK184	JK184 inhibits Gli in the Hedgehog (Hh) pathway with an IC50 of 30 nM in mammalian cells.	Cell Res, 2020, 10.1038/s41422-020-00426-0
E0787	ALLO-2	ALLO-2 is a potent antagonist of both wild-type mouse Smo and drug-resistant D473H mutant human Smo that inhibits Smo agonist inhibited Gli-Luc activity in TM3-Gli-Luc cells with IC50 of 6 nM.
S1182^New	GANT58(NSC75503)	GANT 58 (NSC 75503) is a potent antagonist of GLI-mediated transcription with an IC50 of ≈5 μM. It can be used for research into Ewing Sarcoma and several forms of solid cancer.
E0480	MRT-81	MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells, exerting potent hedgehog (Hh) signalling pathway inhibiting activity.
E0782	MRT 10	MRT-10 inhibits ShhN signalling 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.