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MK-4101 is a novel SMO antagonist of the Hedgehog Pathway. MK-4101 targets the Hh pathway in tumor cells, showing the maximum inhibitory effect on Gli1 MK-4101 also induced deregulation of cell cycle and block of DNA replication in tumors. MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line (Gli_Luc) with IC50 = 1.5 µM and in human KYSE180 oesophageal cancer cells with an IC50 = 1 µM.
MK-4101 was highly efficacious against primary medulloblastoma and BCC developing in the cerebellum and skin of Ptch1(+/-) mice. MK-4101 could be administered orally, showing a good bioavailability (F ≥ 87 %) with low-to-moderate plasma clearance in mice and rats. Moreover, it was well absorbed, and mainly excreted into the bile.
| Cell Experiment | |
|---|---|
| Cell lines | BCC (basal cell carcinoma) cells |
| Preparation method | BCC cells are treated with MK-4101(10 μM) for 72 h and cell cycle is analyzed by FACS monitoring EdU incorporation. |
| Concentrations | 10 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | C57bl/6 mice or Sprague-Dawley rats |
| Formulation | 0.5% methylcellulose in deionized water |
| Dosages | 40 or 80 mg/kg once a day; 80 mg/kg twice a day |
| Administration | oral administration |
| Molecular Weight | 493.47 |
| Formula | C24H24F5N5O |
| CAS Number | 935273-79-3 |
| Solubility (25°C) | DMSO: ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Smo Products |
|---|
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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. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer. |
| Fluticasone
Fluticasone is a corticosteroid and Smo agonist with an IC50 of 99 nM, which activates the Hedgehog signaling pathway and promotes the proliferation of primary neural stem or precursor cells, and can be used in respiratory related studies. |
| HhAntag
HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway. |
| PF-5274857 hydrochloride
PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway. |
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