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SGC 0946 SGC0946 is a potent and selective inhibitor of DOT1L, which potently and selectively kills cells containing an MLL translocation. SGC0946 inhibits DOT1L with an IC50 of 0.3nM in a radioactive enzyme assay and is over 100-fold selective for other HMTs. Synonyms: SGC-0946; SGC 0946; SGC0946. Grades: >98%. CAS No. 1561178-17-3. Molecular formula: C28H40BrN7O4. Mole weight: 618.57. BOC Sciences 10
SGC 0946 (1- [3- [ [ [ (2R, 3S, 4R, 5R) -5- (4-Amino-5-­bromo-7H-pyrrolo [2, 3-d] pyrimidin-7-yl) -3, 4-di hydro­xytetra hydrofuran-2-yl] methyl ] (isopropyl ) amino] pro­pyl] -3- [4- (2, 2-di methyl ethyl) phenyl] urea) Potent DOT1L methyltransferase inhibitor (KD = 0.06nm, IC50 = 0.3nm in a radioactive assay); blocks H3K79 methylation in A431 cells and MCF10A cells (IC50 values are 2.65 and 8.8nm respectively). Inactive at 12 histone methyltransferases and DNMT1. Selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro model of leukemia; lowers levels of MLL target genes HOXA9 and Meis1. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. USBiological 3
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