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Hedgehog/Smoothened
Isoform-selective Products
Signaling Pathway
Hedgehog/Smoothened Products
- All (21)
- Hedgehog/Smoothened Inhibitors (11)
- Hedgehog/Smoothened Antagonists (7)
- 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. |
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| S1146 | Cyclopamine | Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells. |
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|
| 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. |
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|
| 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. |
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|
| 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. |
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|
| 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. |
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| 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. |
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|
| 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. |
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| 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. | ||
| S7138 | BMS-833923 | BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2. |
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| S2157 | Taladegib (LY2940680) | Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2. | ||
| 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. | ||
| 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. | ||
| S7160 | Glasdegib | Glasdegib is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S6565 | JK184 | JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells. | ||
| 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. | ||
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| S2157 | Taladegib (LY2940680) | Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2. | ||
| 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. | ||
| S7160 | Glasdegib | Glasdegib is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S6565 | JK184 | JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells. | ||
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| S7138 | BMS-833923 | BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2. |
|
|
| 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. | ||
| 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 is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells. |
|
|
| 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. |
|
|
| 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. |
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Tags: Smo activity | smoothened pathway | smoothened pathway | smoothened signaling | Smo cancer | Smo pathway | smoothened signaling pathway | smoothened inhibitor review
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