生物活性 | |||
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描述 | MITF (micropthalmia-associated transcription factor) is a lineage restricted basic helix-loop-helix leucine zipper transcription factor that is essential for melanocyte development, function and survival. TRPM-1 (melastatin) is one of the target gene of MITF. ML329 is a selective MITF with IC50 value of 1.2μM in a TRPM-1 promoter activity assay. ML329 exhibited selective anti-proliferative effect on MITF-dependent cells, SK-MEL-5 and MALME-3M, but not A375 cells which is a MITF-independent cell line. Treatment with ML329 reduced reduced the expression of multiple MITF target genes, including pigment-related genes and the cell cycle regulator CDK2. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.05mL 0.61mL 0.30mL |
15.23mL 3.05mL 1.52mL |
30.46mL 6.09mL 3.05mL |
参考文献 |
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[1]Faloon PW, Bennion M, et al. A Small Molecule Inhibitor of the MITF Molecular Pathway. |