Click here to obtain this probe.
A collaboration between the SGC, Eli Lilly, the Icahn School of Medicine at Mount Sinai, and the Ontario Institute for Cancer Research (OICR) has resulted in the discovery of SGC6870, a potent, selective, and cell-active inhibitor of PRMT6. SGC6870 inhibits PRMT6 with IC50 of 77 ± 6 nM and is selective over all other PRMTs and 23 methyltransferases.
SGC6870 inhibits the asymmetric dimethylation of H3R2 by overexpressed PRMT6 in HEK293T cells with an IC50 of 0.8 ± 0.2 microM. SGC6870N is the (S)-enantiomer of SGC6870 and is inactive on PRMT6 and thus an excellent control compound.
Data relating to the discovery of this probe is being prepared for publication. In the meantime, in order to facilitate research by the community we are making this compound available through this website.