A class F G protein-coupled receptor named Smoothened (Smo) transmits the Hedgehog (Hh) signal across the cell membrane. Both canonical and noncanonical pathways make up the Hh signaling pathway. Major Hh molecules like Hh ligands, PTCH, Smo, and GLI are involved in the canonical Hh pathway's operation, whereas Smo or GLI are activated through other pathways in the noncanonical Hh pathway.
The Hh protein ligand binds to its cellular membrane receptor, Patched (PTCH), relieving PTCH-mediated repression of the seven-transmembrane (7TM) protein Smo to start the Hh signaling cascade. The GLI family of transcription factors receive the signal from activated Smo and transmit it to the nucleus, where they translocate to control numerous genes involved in cell differentiation and tissue patterning.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V69128 | (Rac)-SAG | 364590-63-6 | (Rac)-SAG is an isomer of SAG. |
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V22173 | HhAntag | 496794-70-8 | HhAntag is a novel and potent GLI1-mediated transcription inhibitor and SMOantagonistwith anticancer activity. |
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V80355 | IHR-Cy3 | IHR-Cy3 is a potent Smo fluorescence antagonist (inhibitor) with IC50 of 100 nM. | |
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V50986 | KAAD-Cyclopamine | 306387-90-6 | KAAD-Cyclopamine is an inhibitor (blocker/antagonist) of the hedgehog signaling pathway and an antagonist of smoothened. |
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V69130 | LEQ506 (NVP-LEQ506) | 1204975-42-7 | LEQ506 is a second-generation smoothened (smo) inhibitor (antagonist) with IC50s of 2 and 4 nM in humans and mice, respectively. |
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V2018 | MK-4101 HCI | 935273-79-3 | MK-4101 HCl (MK 4101; MK4101)is a novel, potent and selective SMO inhibitor/antagonist of the Hedgehog (Hh) signaling pathway. |
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V2914 | MK-4101 | 935273-79-3 | MK-4101 is a novel, potent and selective SMO inhibitor/antagonist of the Hedgehog (Hh) signaling pathway. |
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V69133 | MRT-10 | 330829-30-6 | MRT-10 is a seven-transmembrane smooth receptor (Smo) antagonist (inhibitor) with IC50 of 0.65 μM in various Hedgehog (Hh) assays. |
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V69132 | MRT-81 | 1263132-08-6 | MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors with IC50 of 41 nM in Shh-light2 cells. |
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V69134 | PF-5274857 hydrochloride | 1613439-62-5 | PF-5274857 HCl is a specific, orally bioactive and BBB (blood-brain barrier) permeable (penetrable) Smo antagonist (inhibitor) with IC50 of 5.8 nM and a Ki of 4.6 nM. |
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V69129 | SAG dihydrochloride | 2702366-44-5 | SAG di-HCl is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). |
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V7879 | SAG hydrochloride | 2095432-58-7 | Smoothened Agonist (SAG) HCl is a potent and cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells. |
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V76538 | SAG-d3 | SAG-d3 is the deuterium labelled form of SAG. | |
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V69131 | SMANT hydrochloride | 1177600-74-6 | SMANT HCl is a Smoothened (Smo) signaling inhibitor. |
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V0099 | Sonidegib phosphate (NVP-LDE-225, Erismodegib, Odomzo) | 1218778-77-8 | Sonidegib phosphate orSonidegib diphosphate, the diphosphate salt of sonidegib (also known as NVP-LDE225, Erismodegib, Sonidegib; trade name ofOdomzo) is a potent and orally bioavailable small-molecule antagonist of the Smoothened (Smo) with potential anticancer activity. |
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