UNC2170, Methyl-lysine Binding Protein 53BP1 Inhibitor

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.

Product information

CAS Number: 2173992-60-2

Molecular Weight: 429.31

Formula: C18H25BrN2O5

Chemical Name: 3-bromo-N-(3-(tert-butylamino)propyl)benzamide maleate

Smiles: CC(C)(C)NCCCNC(=O)C1=CC(Br)=CC=C1.OC(=O)/C=C\C(O)=O

InChiKey: WCAATDGMINWXPJ-BTJKTKAUSA-N

InChi: InChI=1S/C14H21BrN2O.C4H4O4/c1-14(2,3)17-9-5-8-16-13(18)11-6-4-7-12(15)10-11;5-3(6)1-2-4(7)8/h4,6-7,10,17H,5,8-9H2,1-3H3,(H,16,18);1-2H,(H,5,6)(H,7,8)/b;2-1-

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

UNC2170 was used at 10-30 µM final concentration in various in vitro assays.

References:

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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