EN219

EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114. It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8, IC50 = 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 µM. EN219 (1 µM) also interacts with cysteine residues in the tubulin beta1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP human breast cancer cells in a proteomic profiling assay. It has been linked to the bromodomain and extra terminal domain (BET) inhibitor ligand (+)-JQ1 for use as a proteolysis-targeting chimera (PROTAC) to degrade bromodomain-containing protein 4 (BRD4) in 231MFP cells.Formal Name: 1-[3,5-bis(4-bromophenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-chloro-ethanone. CAS Number: 380351-29-1. Molecular Formula: C17H13Br2ClN2O. Formula Weight: 456.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 5 mg/ml, Ethanol: 1 mg/ml. lambdamax: 224, 295, 305 nm. SMILES: BrC(C=C1)=CC=C1C2N(C(CCl)=O)N=C(C3=CC=C(Br)C=C3)C2. InChi Code: 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. InChi Key: CXRHMHAKZPJNKS-UHFFFAOYSA-N.