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SGC-0946 is a protein methyltransferase (PMT) responsible for methylating histone 3 at lysine 79 (H3K79), regulating gene expression, DNA damage repair, and cell cycle control. The Structural Genomics Consortium (SGC) has developed SGC0946, a potent inhibitor of SGC-0946 with a high level of selectivity (over 100-fold) for other PMTs. SGC0946 effectively reduces H3K79 dimethylation in A431 and MCF10A cells, with IC50 values of 2.6nM and 8.8nM, respectively. This inhibitor, derived from the brominated analog of EPZ004777, demonstrates remarkable activity and selectivity in targeting MLL cells, where SGC-0946 is abnormally localized due to its interaction with an oncogenic MLL fusion protein. SGC0649, the negative control for SGC0956, is also available exclusively through the SGC upon request. Overall, SGC0946 exhibits potent inhibitory effects on SGC-0946 and effectively reduces H3K79 dimethylation in cellular models.
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
SGC-0946, 5 mg | sc-473869 | 5 mg | $112.00 |