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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 |
|---|
| GDC-0449 (Vismodegib)
GDC-0449 (Vismodegib) is a potent and specific hedgehog pathway inhibitor with IC50 values of 1.4 and 3.0μM for inhibition of ABCG2 and Pgp respectively. |
| Purmorphamine
Purmorphamine is a small molecule Hh agonist which activates the hedgehog pathway by directly binding to SMO. |
| BMS-833923
BMS-833923 is an orally bioavailable Smoothened antagonist. |
| Halcinonide
Halcinonide is a high potency corticosteroid used in topical preparations as an anti-inflammatory agent. |
| 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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