| S1146 |
Cyclopamine (11-Deoxojervine)
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Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signalling pathway antagonist of Smoothened (Smo) with an IC50 of 46 nM in TM3Hh12 cells.
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Nat Commun, 2025, 16(1):1267
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EMBO Mol Med, 2025, 17(2):336-364
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Development, 2025, 152(8)dev204324
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| S2151 |
Sonidegib (NVP-LDE225, Erismodegib)
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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.
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Nat Commun, 2025, 16(1):5137
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Nat Commun, 2025, 16(1):1267
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Method Protocol, 2025, 8(3)59
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| S7092 |
SANT-1
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SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.
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Nat Commun, 2024, 15(1):9771
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Stem Cell Reports, 2024, 19(7):973-992
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Front Immunol, 2023, 14:1258074
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| S7138 |
BMS-833923
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BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.
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Nat Commun, 2025, 16(1):4983
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Sci Rep, 2022, 12(1):7
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Mol Cancer Res, 2021, molcanres.MCR-21-0257-A.2021
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| S2777 |
PF-5274857
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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.
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Sci Rep, 2022, 12(1):7
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Biol Reprod, 2021, ioab111
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Carcinogenesis, 2020, 41(7):993-1004
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| E0787 |
ALLO-2
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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.
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| S1182New |
GANT58(NSC75503)
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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.
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| E0480 |
MRT-81
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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.
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