pkmt

UNC0224 is a selective inhibitor of G9a with a Ki of 2.6 nM and IC50 of 15 nM. UNC0224 also potently inhibits GLP with assay-dependent IC50 values of 20-58 nM.

UNC0321 is an effective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and with IC50s 9 nM and 6 nM in ECSD and CLOT assays. UNC0321 inhibits GLP with IC50s of 15 nM and 23 nM in ECSD and CLOT assays.

UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).

UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646(UNC 0646) potently blocks G9a/GLP methyltransferase activity in cells (IC50: 10 nM in MCF7 cells) and exhibits low cellular toxicity (EC50: 4.7 μM in MCF7 cells).

ssK36 is a super-substrate peptide derived from the histone methyltransferase (SET) domain protein 2 (SETD2). This peptide was specifically designed for SETD2, a unique PKMT responsible for methylating the 36th lysine residue on histone H3 (H3K36) in human cells, resulting in H3K36me3. Remarkably, ssK36 undergoes methylation by SETD2 at a rate over 100 times faster than the natural substrate H3K36. ssK36 serves as a valuable tool for investigating the catalytic mechanisms of PKMTs, particularly regarding substrate specificity and catalytic efficiency.