For research use only. Not for therapeutic Use.
UNC 669, a ligand for a methyl-lysine binding domain, is a potent L3MBTL1 (IC50=4.2 uM) and L3MBTL3 (3.1 uM) inhibitor[1].
L3MBTL1, a paralogue of Drosophila tumor suppressor lethal(3)malignant brain tumor (l(3)mbt), binds histones in a methylation state-dependent manner and contributes to higher order chromatin structure and transcriptional repression. Similar to L3MBTL1, the closely related protein, L3MBTL3, also contains three MBT repeats and has been shown to play a role in meduloblastoma formation and normal hematopoiesis in humans[1][2].
| Catalog Number | I001207 |
| CAS Number | 1314241-44-5 |
| Synonyms | (5-bromopyridin-3-yl)-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone |
| Molecular Formula | C15H20BrN3O |
| Purity | ≥95% |
| InChI | InChI=1S/C15H20BrN3O/c16-13-9-12(10-17-11-13)15(20)19-7-3-14(4-8-19)18-5-1-2-6-18/h9-11,14H,1-8H2 |
| InChIKey | CQERVFFAOOUFEQ-UHFFFAOYSA-N |
| SMILES | C1CCN(C1)C2CCN(CC2)C(=O)C3=CC(=CN=C3)Br |
| Reference | [1]. James LI, et al. Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3. J Med Chem. 2013 Sep 26;56(18):7358-71. [2]. Trojer P, et al. L3MBTL1, a histone-methylation-dependent chromatin lock. Cell. 2007;129(5):915-928. [3]. Baughman BM, et al. The L3MBTL3 Methyl-Lysine Reader Domain Functions As a Dimer [retracted in: ACS Chem Biol. 2018 Jan 19;13(1):281]. ACS Chem Biol. 2016;11(3):722-728. |
