UNC 926 hydrochloride

UNC926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC50 of 3.9 μM[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

IC50: 3.9 μM (L3MBTL1), 3.2 μM (L3MBTL3), 15.6 μM (L3MBTL4)[1]

UNC926 also exhibits a low micromolar affinity for the close homolog, L3MBTL3 ( IC50 of 3.2 μM), with a decrease in affinity for the other MBT domains and no binding to CBX7[1]. UNC926 (1-25 μM) inhibits binding of the 3xMBT domain to H4K20me1.UNC926 inhibits the association of L3MBTL13xMBT with the appropriate histonepeptides in a dose-dependent manner. UNC926 does not have an effect on the binding of 53BP1 to H4K20me1, demonstrating specificity of UNC926 for L3MBTL1 over 53BP1[1].

[1]. Herold JM, et al. Structure-activity relationships of methyl-lysine reader antagonists. MedChemComm. 2012;3(45):45-51.