Hedgehog/Smoothened

亜型選択性的な製品

シグナル伝達経路

Hedgehog/Smoothenedシグナル伝達経路

Hedgehog/Smoothened製品

  • All (24)
  • Hedgehog/Smoothened阻害剤 (11)
  • Hedgehog/Smoothened拮抗剤(7)
  • Hedgehog/Smoothened作動薬(3)
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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 Metab, 2023, 5(7):1174-1187
Nat Commun, 2023, 14(1):7161
Cell Rep, 2023, S2211-1247(23)01614-5
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, 2024, 15(1):987
Dis Model Mech, 2024, 17(2)dmm050323
Chinese Journal of Tissue Engineering Research, 2024, Vol. 28 ›› Issue (26): 4194-4201.
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.
Acta Pharm Sin B, 2023, 13(6):2601-2612
Cell Death Dis, 2023, 14(7):461
Cell Death Dis, 2023, 14(12):830
S7779 SAG (Smoothened Agonist) HCl SAG (Smoothened Agonist) HClは1種の細胞浸透性Smoothened (Smo)の作動剤で、Shh-LIGHT2細胞の中でEC50 値は3 nMです。
Nat Commun, 2023, 14(1):4346
Biofabrication, 2023, 15(4).
Cell Rep, 2023, S2211-1247(23)01614-5
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.
Cell Death Dis, 2024, 15(1):56
Nat Commun, 2023, 14(1):2696
Cell Rep, 2023, S2211-1247(23)01614-5
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, 2024, 15(1):987
Neural Regen Res, 2024, 19(1):205-211
Regen Ther, 2024, 25:229-237
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.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Cell Infect Microbiol, 2022, 12:864912
Front Cell Infect Microbiol, 2022, 12:1074903
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.
Nat Commun, 2022, 13(1):2407
Sci Rep, 2022, 12(1):7
Hum Cell, 2022, 10.1007/s13577-022-00796-0
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 Res, 2023, 33(6):421-433
Biofabrication, 2023, 15(4).
Aging (Albany NY), 2023, 10.18632/aging.205110
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.
Elife, 2023, 12e80040
Int J Mol Sci, 2022, 23(24)15573
Int J Mol Sci, 2022, 23(23)14500
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.
Leukemia, 2023, 37(8):1649-1659
Front Cell Dev Biol, 2021, 9:662868
Genome Med, 2020, 18;12(1):17
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.

Mol Cell, 2022, S1097-2765(22)00327-6
J Cell Sci, 2022, 135(21)jcs259999
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
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.
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.
S7779 SAG (Smoothened Agonist) HCl SAG (Smoothened Agonist) HClは1種の細胞浸透性Smoothened (Smo)の作動剤で、Shh-LIGHT2細胞の中でEC50 値は3 nMです。
Nat Commun, 2023, 14(1):4346
Biofabrication, 2023, 15(4).
Cell Rep, 2023, S2211-1247(23)01614-5
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, 2024, 15(1):987
Neural Regen Res, 2024, 19(1):205-211
Regen Ther, 2024, 25:229-237
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 Res, 2023, 33(6):421-433
Biofabrication, 2023, 15(4).
Aging (Albany NY), 2023, 10.18632/aging.205110
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 Metab, 2023, 5(7):1174-1187
Nat Commun, 2023, 14(1):7161
Cell Rep, 2023, S2211-1247(23)01614-5
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.
Acta Pharm Sin B, 2023, 13(6):2601-2612
Cell Death Dis, 2023, 14(7):461
Cell Death Dis, 2023, 14(12):830
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.
Front Cell Infect Microbiol, 2023, 13:1128000
Front Cell Infect Microbiol, 2022, 12:864912
Front Cell Infect Microbiol, 2022, 12:1074903
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.
Elife, 2023, 12e80040
Int J Mol Sci, 2022, 23(24)15573
Int J Mol Sci, 2022, 23(23)14500
S7160 Glasdegib Glasdegib is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
Leukemia, 2023, 37(8):1649-1659
Front Cell Dev Biol, 2021, 9:662868
Genome Med, 2020, 18;12(1):17
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.

Mol Cell, 2022, S1097-2765(22)00327-6
J Cell Sci, 2022, 135(21)jcs259999
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, 2024, 15(1):987
Dis Model Mech, 2024, 17(2)dmm050323
Chinese Journal of Tissue Engineering Research, 2024, Vol. 28 ›› Issue (26): 4194-4201.
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.
Cell Death Dis, 2024, 15(1):56
Nat Commun, 2023, 14(1):2696
Cell Rep, 2023, S2211-1247(23)01614-5
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.
Nat Commun, 2022, 13(1):2407
Sci Rep, 2022, 12(1):7
Hum Cell, 2022, 10.1007/s13577-022-00796-0
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.
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は1種の細胞浸透性Smoothened (Smo)の作動剤で、Shh-LIGHT2細胞の中でEC50 値は3 nMです。
Nat Commun, 2023, 14(1):4346
Biofabrication, 2023, 15(4).
Cell Rep, 2023, S2211-1247(23)01614-5
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, 2024, 15(1):987
Neural Regen Res, 2024, 19(1):205-211
Regen Ther, 2024, 25:229-237
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 Res, 2023, 33(6):421-433
Biofabrication, 2023, 15(4).
Aging (Albany NY), 2023, 10.18632/aging.205110

Hedgehog/Smoothened阻害剤の選択性比較

Tags: Smo activity | smoothened pathway | smoothened pathway | smoothened signaling | Smo cancer | Smo pathway | smoothened signaling pathway | smoothened inhibitor review