biological activity | UNC926 is a methyl-lysine (Kme) reader domain inhibitor, which can specifically inhibit L3MBTL1, and its IC50 is 3.9 μM. |
target | TargetValue L3MBTL1 () 3.9 μM(Kd) |
Target | Value |
L3MBTL1
()
| 3.9 μM(Kd) |
in vitro study | UNC926 also exhibits a low micromolar affinity for the close homolog, L3MBTL3 ( IC 50 of 3.2 μM), with a decrease in affinity for the other MBT domains and no binding to CBX7. UNC926 (1-25μM) inhibits binding of the 3xMBT domain to H4K20me1.UNC926 inhibits the association of L3MBTL13xMBT with the appropriate histonepeptides in a pose-dependent manner. UNC926 does not have an effect on the binding of 53BP1 to H4K20me1, demonstrating specificity of UNC926 for L3MBTL1 over 53BP1. |
use | UNC-926 is a methyl-lysine reader antagonist; binds to the MBT domain of the L3MBTL1 protein (Kd = 3.9 μM). UNC-926 selectively inhibits the interaction between L3MBTL13XMBT-H4K20me1 in a peptide pull down say. |