MK-4101,935273-79-3

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MK-4101

CAS No. : 935273-79-3

MCE 国际站：MK-4101

产品活性：MK-4101 是一种 SMO 拮抗剂 (对 293 细胞的 IC₅₀ 为 1.1 µM)，也是一种有效的 hedgehog 途径抑制剂 (对小鼠细胞的 IC₅₀ 为 1.5 µM；对 KYSE180 食管癌细胞的 IC₅₀ 为 1 µM)。MK-4101 具有强大的抗肿瘤活性，能抑制肿瘤细胞增殖并诱导细胞凋亡。

研究领域：Stem Cell/Wnt  |  Apoptosis

作用靶点：Smo  |  Apoptosis  |  Hedgehog

In Vitro: MK-4101 inhibits Hh signaling both in a reporter gene assay in an engineered mouse cell line with an IC₅₀ of 1.5 µM, and in human KYSE180 oesophageal cancer cells with an IC₅₀ of 1 µM. MK-4101 displaces a fluorescently-labeled cyclopamine derivative from 293 cells expressing recombinant human SMO with an IC₅₀ of 1.1 µM, implying that the compound binds to SMO. MK4101 also inhibits the proliferation of medulloblastoma cells derived from neonatallyirradiated Ptch1^-/+ mice in vitro with an IC₅₀ of 0.3 µM.
MK-4101 (10 µM; 60 hours, 72 hours; medulloblastoma or BCC cells) treatment shows cell cycle arrest with a nearly complete disappearance of the S phase subpopulation, a prominent increase of the G1 population and, to a minor extent, of the G2 population.
MK-4101 (10 µM; medulloblastoma or BCC cells) treatment significantly reduces cyclin D1 protein and accumulation of cyclin B1 protein.

In Vivo: MK-4101 (40-80 mg/kg; oral administration; for 3.5 weeks; CD1 nude female mice) treatment shows tumor growth inhibition (40 and 80 mg/kg ) and tumor regression at the highest dose (80 mg/kg). MK-4101 treatment shows a dose-dependent down-regulation of Gli1 mRNA. The maximum effect for tumor inhibition and hedgehog pathway downregulation is achieved at 80 mg/kg.

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