ML216 化学特性,用途語,生産方法
説明
Bloom (BLM) helicase is a DNA unwinding enzyme important for DNA repair in the homologous recombination pathway. Mutations of the BLM gene result in reduced BLM helicase activity that is associated with the rare genetic disorder, Bloom’s Syndrome, and a predisposition to developing cancer. ML-
216 is the first identified small molecule inhibitor of BLM helicase (IC
50 = 1.8 μM) that is 28-
fold selective against the related helicases RECQ1, RECQ5, and
E. coli UvrD (IC
50s ≥ 50 μM). At 25-
50 μM, ML-
216 has been shown to dose-
dependently inhibit the proliferation of BLM-
expressing PSNF5 fibroblast cells but not BLM-
deficient PSNG13 fibroblast cells.
使用
ML216 has been used in cell proliferation assays.
Biochem/physiol Actions
ML216 is a membrane permeable selective inhibitor of Bloom (BLM) helicase, a member of the RecQ DNA helicase family. Bloom′s syndrome, caused by a mutation in BLM, is associated with susceptibility to cancer, growth retardation, immunodeficiency, sunlight sensitivity, and fertility defects. ML216 is selective for BLM over other members of the RecQ family, especially in vivo, and appears to act at the BLM-nucleic acid substrate binding site, inhibiting DNA binding and blocking BLM′s helicase activity. ML216 could be useful in studies of tumor cells depending on the ALT (alternative lengthening of telomeres) mechanism for telomere maintenance rather than on telomerase, which are proposed to be susceptible to BLM inhibition.
ML216 上流と下流の製品情報
原材料
準備製品