ML329 inhibits the expression of numerous micropthalmia-associated transcription factor (MITF) target genes and blocks the proliferation of numerous cell lines that require MITF for proliferation. It could directly or indirectly interact with MITF or components of the MITF regulatory network. As a transcription factor that regulates cell cycle and pigmentation, interference of MITF with it will be useful in characterizing the specific roles of MITF in melanoma and validate blockade of MITF function as a potential treatment of melanoma. It shows specific activity against the MITF -dependent cells, primary melanocytes but no effect on the viability in A375 cells. It reduces the expression of multiple MITF target genes, including pigment-related genes and the cell cycle regulator CDK2. As a tool compound, it will be useful in elucidating the role of MITF in melanocyte lineage development and in melanoma disease progression.
