UNC2170, Methyl-lysine Binding Protein 53BP1 Inhibitor


Catalog No. size PriceQuantity
M60260-2S 2 mg solid $99
M60260-10S 10mg solid $391

Description

Product Information
Molecular Weight: 429.31
Formula: C14H21BrN2O.C4H4O4
Purity: ≥98%
CAS#: 2173992-60-2
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.

 

Biological Activity:

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

Reference:

  • 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. 



Products are for research use only. Not for human use. 

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