|Solubility:||DMSO up to 100 mM|
|Chemical Name:||3-bromo-N-(3-(tert-butylamino)propyl)benzamide maleate|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
UNC2170 is a selective and cell permeable methyl-lysine binding protein 53BP1 antagonist with micromolar activity. It displays >17-fold selectivity for 53BP1 as compared to other methyl-lysine (Kme) binding proteins tested. Structural studies revealed that the tert-butyl amine of UNC2170 anchors the compound in the methyl-lysine (Kme) binding pocket of 53BP1, making it competitive with endogenous Kme substrates. X-ray crystallography also demonstrated that UNC2170 binds at the interface of two tudor domains of a 53BP1 dimer. It functions as a 53BP1 antagonist in cellular lysates and shows cellular activity by suppressing class switch recombination, a process which requires a functional 53BP1 tudor domain.
How to Use:
In vitro: UNC2170 was used at 10-30 µM final concentration in various in vitro assays.
In vivo: n/a
- 1. Perfetti MT, et al. Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1. (2015) ACS Chem Biol. 10(4):1072-81.
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