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ML216 ?98% (HPLC). Group: Fluorescence/luminescence spectroscopy. Alfa Chemistry Analytical Products 3
ML216 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 (IC50 = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s ≥ 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. Synonyms: ML 216; ML-216; CID-49852229; CID49852229; CID 49852229. Grades: >98%. CAS No. 1430213-30-1. Molecular formula: C15H9F4N5OS. Mole weight: 383.32. BOC Sciences 9
BLM Helicase Inhibitor, ML216 (ML-216, 1- (4-Fluoro-3- (trifluoromethyl) phenyl) -3- (5- (pyridin-4-yl) -1, 3, 4-thiadiazol-2-yl) urea) A cell-permeable pyridinyl-thiadiazolylurea compound that selectively blocks Bloom's syndrome protein (BLM) helicase activity of both full-length as well as truncated BLM636-1298 forms (IC50 = 2.98 and 0.97uM, respectively). Competes with and reversibly blocks DNA binding to BLM. However, the inhibition appears to be non-competitive with respect to ATP. Exhibits anti-proliferative activity in cells expressing BLM, but not in those lacking BLM. Induces sister chromatid exchanges (SCEs) and enhances the sensitivity of BLM containing PSNF5 cells to aphidicolin without affecting PSNG13 cells that are devoid of BLM. Displays favorable microsomal (T1/2 > 1.2h) and plasma stability (~100% at 5h). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H?F?N?OS. US Biological Life Sciences. USBiological 4
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