A cell-permeable pyrrolidinyl-piperidinyl-benzamide that effectively competes against H4K20Me2 peptide for L3MBTL3 binding by targeting the first two L3MBTL3 MBT domains (Kd = 120nM in binding studies using recombinant 3MBT fragment), while exhibiting much reduced potency against L3MBTL1-H4K20Me1, 53BP1-H4K20Me2, MBTD1-H4K20Me1, or L3MBTL4-H2AK36Me1 interaction (IC50 ≥2uM; [peptide] = 150nM). Shown to increase GFP-L3MBTL fusion nucleus mobility (10nM to 1uM) in HEK293 transfectants. X-ray structural analysis reveals two 3MBT are bridged together by two UNC1215 molecules in a reciprocal fashion.
Solubility:DMSO
Primary Target:Kme binding ligand of L3MBTL3
Primary Target IC50:40nM
Primary Target Ki:0.12u
Molar Mass:529.7
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months after receipt at -20°C. Reconstitute with sterile buffer or ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
