Hedgehog/Smoothened

Choose Selective Hedgehog/Smoothened Inhibitors

Hedgehog/Smoothened Signaling Pathway Map

Hedgehog/Smoothened Signaling Pathways

Hedgehog/Smoothened Products

  • All (19)
  • Hedgehog/Smoothened Inhibitors (10)
  • Hedgehog/Smoothened Antibodie (1)
  • Hedgehog/Smoothened Antagonists (5)
  • Hedgehog/Smoothened Agonists (3)
  • New Hedgehog/Smoothened Products
Catalog 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, 2022, 13(1):1439
Neuro Oncol, 2022, noac001
Front Immunol, 2022, 13:841045
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
Sci Rep, 2019, 9(1):1897
S2476 Itraconazole (R 51211) Itraconazole (R 51211) 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.
Microbiol Spectr, 2022, 10(1):e0200721
BMC Microbiol, 2022, 22(1):21
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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
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
S7160 Glasdegib (PF-04449913) Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
Front Cell Dev Biol, 2021, 9:662868
Genome Med, 2020, 18;12(1):17
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.
Cell Death Dis, 2022, 13(2):136
Front Immunol, 2022, 13:841045
Future Med Chem, 2022, 14(7):479-500
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
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.
FASEB J, 2020, 10.1096/fj.201901852RR
Front Pharmacol, 2019, 10:290
PLoS One, 2019, 14(5):e0216642
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.
A5208 ULK3 Rabbit Recombinant mAb ULK3 Rabbit Recombinant mAb detects endogenous level of total ULK3.
S1146 Cyclopamine Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.
Cell Rep, 2022, 38(7):110379
Cell Death Dis, 2022, 13(2):136
Oxid Med Cell Longev, 2022, 2022:9955677
S2151 Sonidegib (NVP-LDE225) Sonidegib (Erismodegib, NVP-LDE225) 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.
J Mol Cell Biol, 2022, mjab082
Biochem Pharmacol, 2022, 199:115009
CNS Neurosci Ther, 2022, 10.1111/cns.13835
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
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.
Sci Rep, 2022, 12(1):7
Adv Sci (Weinh), 2021, e2103495
ACS Appl Mater Interfaces, 2021, 13(2):3199-3208
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
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.
Nat Commun, 2022, 13(1):1439
Oxid Med Cell Longev, 2022, 2022:9955677
Cancer Cell, 2021, 39(3):407-422.e13
S6384New Smoothened Agonist (SAG)

Smoothened Agonist (SAG) is potent agonist of Smoothened (Smo). Smoothened Agonist induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM.

Nat Commun, 2022, 13(1):2387
J Nat Med, 2022, 10.1007/s11418-022-01603-8
EMBO Rep, 2021, e53015
S7779 Smoothened Agonist (SAG) HCl Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
Nat Commun, 2022, 13(1):2387
EMBO Mol Med, 2022, e14990
Front Immunol, 2022, 13:841045
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, 2022, 13(1):1439
Neuro Oncol, 2022, noac001
Front Immunol, 2022, 13:841045
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
Sci Rep, 2019, 9(1):1897
S2476 Itraconazole (R 51211) Itraconazole (R 51211) 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.
Microbiol Spectr, 2022, 10(1):e0200721
BMC Microbiol, 2022, 22(1):21
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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
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
S7160 Glasdegib (PF-04449913) Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
Front Cell Dev Biol, 2021, 9:662868
Genome Med, 2020, 18;12(1):17
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.
Cell Death Dis, 2022, 13(2):136
Front Immunol, 2022, 13:841045
Future Med Chem, 2022, 14(7):479-500
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
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.
FASEB J, 2020, 10.1096/fj.201901852RR
Front Pharmacol, 2019, 10:290
PLoS One, 2019, 14(5):e0216642
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.
A5208 ULK3 Rabbit Recombinant mAb ULK3 Rabbit Recombinant mAb detects endogenous level of total ULK3.
S1146 Cyclopamine Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.
Cell Rep, 2022, 38(7):110379
Cell Death Dis, 2022, 13(2):136
Oxid Med Cell Longev, 2022, 2022:9955677
S2151 Sonidegib (NVP-LDE225) Sonidegib (Erismodegib, NVP-LDE225) 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.
J Mol Cell Biol, 2022, mjab082
Biochem Pharmacol, 2022, 199:115009
CNS Neurosci Ther, 2022, 10.1111/cns.13835
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
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.
Sci Rep, 2022, 12(1):7
Adv Sci (Weinh), 2021, e2103495
ACS Appl Mater Interfaces, 2021, 13(2):3199-3208
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
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.
Nat Commun, 2022, 13(1):1439
Oxid Med Cell Longev, 2022, 2022:9955677
Cancer Cell, 2021, 39(3):407-422.e13
S6384New Smoothened Agonist (SAG)

Smoothened Agonist (SAG) is potent agonist of Smoothened (Smo). Smoothened Agonist induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM.

Nat Commun, 2022, 13(1):2387
J Nat Med, 2022, 10.1007/s11418-022-01603-8
EMBO Rep, 2021, e53015
S7779 Smoothened Agonist (SAG) HCl Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
Nat Commun, 2022, 13(1):2387
EMBO Mol Med, 2022, e14990
Front Immunol, 2022, 13:841045
S6384New Smoothened Agonist (SAG)

Smoothened Agonist (SAG) is potent agonist of Smoothened (Smo). Smoothened Agonist induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM.

Nat Commun, 2022, 13(1):2387
J Nat Med, 2022, 10.1007/s11418-022-01603-8
EMBO Rep, 2021, e53015
Tags: Smo activity | smoothened pathway | smoothened pathway | smoothened signaling | Smo cancer | Smo pathway | smoothened signaling pathway | smoothened inhibitor review