Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MK-4101, an effective inhibitor of the Hedgehog pathway, has anti-tumor activity through the induction of extensive apoptosis and inhibition of proliferation in tumor cells.
説明 | MK-4101, an effective inhibitor of the Hedgehog pathway, has anti-tumor activity through the induction of extensive apoptosis and inhibition of proliferation in tumor cells. |
ターゲット&IC50 | Mouse cells:1.5 µM (IC50), KYSE180 oesophageal cancer cells:1 µM (IC50), HEK293 cells:1.1 µM (IC50) |
In vitro | 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. Furthermore, MK-4101 displaced a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC50 = 1.1 μM. MK-4101 arrests cells in G1 and G2 phases[1]. |
In vivo | MK-4101 has robust antitumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells. MK-4101 is highly efficacious against primary medulloblastoma and basal cell carcinoma(BCC) developing in the cerebellum and skin of Ptch1+/- mice. Pharmacokinetics of MK-4101 shows that it 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[1]. |
キナーゼ試験 | Luciferase assays: After various compound treatments, cells are lysed in luciferase lysis buffer and assayed for luciferase activity using the ONE-Glo luciferase assay system. All luciferase activities are normalized to protein concentration determined by Bradford assay. |
細胞研究 | BCC cells are treated with MK-4101(10 μM) for 72 h and cell cycle is analyzed by FACS monitoring EdU incorporation. (Only for Reference) |
分子量 | 493.47 |
分子式 | C24H24F5N5O |
CAS No. | 935273-79-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 60 mg/mL (121.6 mM)
DMSO: 92 mg/mL (186.4 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. 詳細
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MK-4101 935273-79-3 Apoptosis GPCR/G Protein Stem Cells Smo Hedgehog/Smoothened MK4101 inhibit Smoothened Hedgehog MK 4101 Inhibitor inhibitor