| Molecular Weight: | 338.24 |
| Formula: | C15H20BrN3O |
| Purity: | ≥ 98% |
| CAS#: | 314241-44-5 |
| Solubility: | DMSO up to 50 mM |
| Chemical Name: | (2-(phenylamino)-1,4-phenylene)bis((4-(pyrrolidin-1-yl)piperidin-1-yl)methanone) |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
UNC669 is a potent and selective small molecule inhibitor for the methyl-lysine (Kme) reading function of L3MBTL1, a member of the malignant brain tumor (MBT) family of chromatin-interacting transcriptional repressors. UNC669 binds L3MBTL1 with a Kd of 5±1 μM (IC50 = 6 ±0.5 μM), exhibiting 5-fold greater affinity than the cognate peptide H4K20Me1, 6-fold selective over its close homologue L3MBTL3 and 10-fold selective over L3MBTL4. The first cocrystal structure of UNC669 bound to L3MBTL1 was determined and provides new insights into binding requirements for further ligand design. UNC669 can serve as a useful chemical tool to interrogate the functions of MBT proteins and probe methyl-lysine reader proteins as a target class.
How to Use:
- In vitro: UNC1215 was used at 10-25 µM final concentration in vitro and in cellular assays.
- In vivo: n/a
Reference:
- 1. Herold JM, et al. Small-molecule ligands of methyl-lysine binding proteins. (2011) J Med Chem. 54(7):2504-11.
Products are for research use only. Not for human use.
