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UNC0631 demonstrates remarkable potency and selectivity as an inhibitor of G9a activity both in vitro and in cellular contexts. In vitro, it exhibits a potent inhibitory effect on G9a activity with an IC50 of 4 nM, effectively impeding G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells with an IC50 of 25 nM. Its inhibitory prowess extends to various cancer cell lines and the human fetal lung IMR-90 cell line, effectively targeting G9a/GLP activity. UNC0631 stands out as a novel G9a inhibitor, showcasing exceptional potency across multiple cell lines while maintaining a significant separation between functional efficacy and cellular toxicity. The protein lysine methyltransferase G9a plays a pivotal role in transcriptional repression, employing H3K9me2 dimethylation of chromatin as well as nonhistone proteins.
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
UNC0631, 5 mg | sc-397011 | 5 mg | $149.00 |