UNC-2170 maleate

CAS NO.：2173992-60-2
Empirical Formula: C18H25BrN2O5
Molecular Weight: 429.31
Update Date: 2025-04-17 18:22:24

What is UNC-2170 maleate?

Description

p53-Binding protein 1 (53BP1) binds to dimethylated lysine 20 on histone 4 (H4K20me2) via tandem tudor domains on a 53BP1 homodimer.¹ This interaction is an important part of the DNA damage response.¹ UNC2170 is a micromolar ligand of 53BP1 that binds to a pocket formed by the tandem tudor domains.² It displays at least 17-fold selectivity for 53BP1 over other methyl-lysine binding proteins.² UNC2170 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.²

References

1. Botuyan, M.V., Lee, J., Ward, I.M., et al. Structural basis for the methylation state-specific recognition for histone H4-K20 by 53BP1 and Crb2 in DNA repair Cell 127(7),1361-1373(2006).
2. Perfetti, M.T., Baughman, B.M., Dickson, B.M., et al. Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1 ACS Chem. Biol. 10(4),1072-1081(2015).

Properties of UNC-2170 maleate

solubility	DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 1 mg/ml; PBS (pH 7.2): 1 mg/ml
form	A crystalline solid

Safety information for UNC-2170 maleate

Computed Descriptors for UNC-2170 maleate

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