Target & Activity
| Target | Activity | Value |
|---|---|---|
| EHMT1/GLP/KMT1D | IC50 | 20-58 nM |
| G9a | IC50 | 15 nM |
| G9a | Ki | 2.6 nM |
| G9a | Kd | 23 nM |
Cellular Effect
| Cell Line | Activity | Value | Description | Reference |
|---|---|---|---|---|
| MDA-MB-231 | IC50 | > 5 μM | Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay | [PMID: 21780790] |
| MDA-MB-231 | EC50 | 34 μM | Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay | [PMID: 21780790] |
| Sf9 | IC50 | 23 nM | Inhibition of N-terminal GST tagged human recombinant EHMT1 (794 to 1294 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 m | [PMID: 31350126] |
| Sf9 | IC50 | 60 nM | Inhibition of N-terminal GST tagged human recombinant EHMT2 (785 to 1210 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 m | [PMID: 31350126] |