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Hedgehog/Smoothened

Isoform-selective Products

Hedgehog Smoothened GLI

Signaling Pathway

Hedgehog/Smoothened Products

All (23)
Hedgehog/Smoothened Inhibitors (11)
Hedgehog/Smoothened Antagonists (8)
Hedgehog/Smoothened Agonists (3)
New Hedgehog/Smoothened Products

Catalog No.	Product Name	Information	Product Use Citations
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):1092 Nat Commun, 2025, 16(1):1267 J Exp Clin Cancer Res, 2025, 44(1):22
S1146	Cyclopamine	Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.	Nat Commun, 2025, 16(1):1267 EMBO Mol Med, 2025, 17(2):336-364 Development, 2025, 152(3)DEV204214
S8075	GANT61	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 J Exp Clin Cancer Res, 2025, 44(1):22 EMBO Mol Med, 2025, 17(2):336-364
S7779	SAG (Smoothened Agonist) HCl	SAG (Smoothened Agonist) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.	Nat Commun, 2025, 16(1):1267 EMBO J, 2025, 44(9):2541-2565 EMBO J, 2025, 10.1038/s44318-025-00399-z
S2151	Sonidegib	Sonidegib is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.	Nat Commun, 2025, 16(1):1267 EBioMedicine, 2024, 101:105026 Cell Death Dis, 2024, 15(10):739
S3042	Purmorphamine	Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.	Development, 2025, 152(3)DEV204214 Nat Commun, 2024, 15(1):987 J Adv Res, 2024, S2090-1232(24)00106-1
S2476	Itraconazole	Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.	Infect Drug Resist, 2025, 18:783-789 iScience, 2024, 27(10):110862 ACS Infect Dis, 2024, 10(11):3973-3993
S7092	SANT-1	SANT-1 directly binds to Smoothened (Smo) receptor with K_d of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.	Nat Commun, 2024, 15(1):9771 Stem Cell Reports, 2024, 19(7):973-992 Front Immunol, 2023, 14:1258074
S6384	SAG (Smoothened Agonist)	SAG (Smoothened Agonist) is a potent agonist of Smoothened (Smo). Smoothened Agonist induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM.	Cell Rep, 2025, 44(5):115597 Open Biol, 2025, 15(4):240342 EBioMedicine, 2024, 101:105026
S7138	BMS-833923	BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.	Sci Rep, 2022, 12(1):7 Mol Cancer Res, 2021, molcanres.MCR-21-0257-A.2021 Carcinogenesis, 2020, 41(7):993-1004
S2157	Taladegib (LY2940680)	Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.	Sci Rep, 2022, 12(1):7 Carcinogenesis, 2020, 41(7):993-1004 Front Pharmacol, 2019, 10:89
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 Int J Mol Sci, 2025, 26(5)2138 Hum Exp Toxicol, 2025, 44:9603271251332251
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.	Sci Rep, 2022, 12(1):7 Biol Reprod, 2021, ioab111 Carcinogenesis, 2020, 41(7):993-1004
S7160	Glasdegib	Glasdegib is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.	iScience, 2024, 27(10):110862 Leukemia, 2023, 37(8):1649-1659 Front Cell Dev Biol, 2021, 9:662868
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.	Sci Rep, 2022, 12(1):7 Neurochem Int, 2021, 146:105042
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. Ciliobrevin D 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
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
F2408^New	ARL 13B mAb
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 IC50 of ≈5 μM. It can be used for research in 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) signaling pathway inhibiting activity.
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.
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):1092 Nat Commun, 2025, 16(1):1267 J Exp Clin Cancer Res, 2025, 44(1):22
S8075	GANT61	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 J Exp Clin Cancer Res, 2025, 44(1):22 EMBO Mol Med, 2025, 17(2):336-364
S2476	Itraconazole	Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.	Infect Drug Resist, 2025, 18:783-789 iScience, 2024, 27(10):110862 ACS Infect Dis, 2024, 10(11):3973-3993
S2157	Taladegib (LY2940680)	Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.	Sci Rep, 2022, 12(1):7 Carcinogenesis, 2020, 41(7):993-1004 Front Pharmacol, 2019, 10:89
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 Int J Mol Sci, 2025, 26(5)2138 Hum Exp Toxicol, 2025, 44:9603271251332251
S7160	Glasdegib	Glasdegib is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.	iScience, 2024, 27(10):110862 Leukemia, 2023, 37(8):1649-1659 Front Cell Dev Biol, 2021, 9:662868
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.	Sci Rep, 2022, 12(1):7 Neurochem Int, 2021, 146:105042
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. Ciliobrevin D 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
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.
S1146	Cyclopamine	Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.	Nat Commun, 2025, 16(1):1267 EMBO Mol Med, 2025, 17(2):336-364 Development, 2025, 152(3)DEV204214
S2151	Sonidegib	Sonidegib is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.	Nat Commun, 2025, 16(1):1267 EBioMedicine, 2024, 101:105026 Cell Death Dis, 2024, 15(10):739
S7092	SANT-1	SANT-1 directly binds to Smoothened (Smo) receptor with K_d of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.	Nat Commun, 2024, 15(1):9771 Stem Cell Reports, 2024, 19(7):973-992 Front Immunol, 2023, 14:1258074
S7138	BMS-833923	BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.	Sci Rep, 2022, 12(1):7 Mol Cancer Res, 2021, molcanres.MCR-21-0257-A.2021 Carcinogenesis, 2020, 41(7):993-1004
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.	Sci Rep, 2022, 12(1):7 Biol Reprod, 2021, ioab111 Carcinogenesis, 2020, 41(7):993-1004
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 IC50 of ≈5 μM. It can be used for research in 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) signaling pathway inhibiting activity.
S7779	SAG (Smoothened Agonist) HCl	SAG (Smoothened Agonist) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.	Nat Commun, 2025, 16(1):1267 EMBO J, 2025, 44(9):2541-2565 EMBO J, 2025, 10.1038/s44318-025-00399-z
S3042	Purmorphamine	Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.	Development, 2025, 152(3)DEV204214 Nat Commun, 2024, 15(1):987 J Adv Res, 2024, S2090-1232(24)00106-1
S6384	SAG (Smoothened Agonist)	SAG (Smoothened Agonist) is a potent agonist of Smoothened (Smo). Smoothened Agonist induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM.	Cell Rep, 2025, 44(5):115597 Open Biol, 2025, 15(4):240342 EBioMedicine, 2024, 101:105026
F2408^New	ARL 13B mAb
S1182^New	GANT58(NSC75503)	GANT 58 (NSC 75503) is a potent antagonist of GLI-mediated transcription with IC50 of ≈5 μM. It can be used for research in Ewing Sarcoma and several forms of solid cancer.

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