In 2012,Yuan, Yuan; Wang, Qiu; Paulk, Joshiawa; Kubicek, Stefan; Kemp, Melissa M.; Adams, Drew J.; Shamji, Alykhan F.; Wagner, Bridget K.; Schreiber, Stuart L. published 《A Small-Molecule Probe of the Histone Methyltransferase G9a Induces Cellular Senescence in Pancreatic Adenocarcinoma》.ACS Chemical Biology published the findings.Application In Synthesis of Methyl 4-fluoro-3-nitrobenzoate The information in the text is summarized as follows:
Post-translational modifications of histones alter chromatin structure and play key roles in gene expression and specification of cell states. Small mols. that target chromatin-modifying enzymes selectively are useful as probes and have promise as therapeutics, although very few are currently available. G9a (also named euchromatin histone methyltransferase 2 (EHMT2)) catalyzes methylation of lysine 9 on histone H3 (H3K9), a modification linked to aberrant silencing of tumor-suppressor genes, among others. Here, we report the discovery of a novel histone methyltransferase inhibitor, BRD4770 (I). This compound reduced cellular levels of di- and trimethylated H3K9 without inducing apoptosis, induced senescence, and inhibited both anchorage-dependent and -independent proliferation in the pancreatic cancer cell line PANC-1. ATM-pathway activation, caused by either genetic or small-mol. inhibition of G9a, may mediate BRD4770-induced cell senescence. BRD4770 may be a useful tool to study G9a and its role in senescence and cancer cell biol. In the part of experimental materials, we found many familiar compounds, such as Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9Application In Synthesis of Methyl 4-fluoro-3-nitrobenzoate)
Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.Application In Synthesis of Methyl 4-fluoro-3-nitrobenzoate
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