For research use only. Not for therapeutic Use.
EN219 is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC50 of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination[1].
EN219 (1 μM; 90 min) interacts with RNF114 C8, TUBB1 C201, HSPD1 C442, and HIST1H3A C97 demonstrated by isotopic tandem orthogonal proteolysisABPP (isoTOP-ABPP) analysis[1].
Catalog Number | I026833 |
CAS Number | 380351-29-1 |
Synonyms | 1-[3,5-bis(4-bromophenyl)-3,4-dihydropyrazol-2-yl]-2-chloroethanone |
Molecular Formula | C17H13Br2ClN2O |
Purity | ≥95% |
InChI | InChI=1S/C17H13Br2ClN2O/c18-13-5-1-11(2-6-13)15-9-16(22(21-15)17(23)10-20)12-3-7-14(19)8-4-12/h1-8,16H,9-10H2 |
InChIKey | CXRHMHAKZPJNKS-UHFFFAOYSA-N |
SMILES | C1C(N(N=C1C2=CC=C(C=C2)Br)C(=O)CCl)C3=CC=C(C=C3)Br |
Reference | [1]. Luo M, et al. Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product function. Cell Chem Biol. 2021 Apr 15;28(4):559-566.e15. |