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Description: LLY-284 is a negative control for LLY-283. It is a diastereomer of LLY-283 but was much less active. LLY-283 is the first potent and selective SAM-competitive chemical probe for PRMT5 (protein arginine methyltransferase 5). In a biochemical assay, LLY-283 inhibits the PRMT5 enzyme activity with an IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, it exhibits more than 100-fold selectivity for PRMT5 than other histone methyltransferases and non-epigenetic targets. PRMTs binds to the lysine or arginine residues of substrate proteins via the substrate binding groove and SAM via the cofactor binding site.
References: ACS Med. Chem. Lett. (2018) DOI: 10.1021/acsmedchemlett.8b00014
Related CAS#:2040291-27-6 (LLY-283)
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