EN219 是一种中等选择性的合成共价配体，针对 RNF114 的 N 端半胱氨酸 (C8)，IC50 为 470 nM。 EN219 抑制 RNF114 介导的自身泛素化和 p21 泛素化。
货号:ajcx25226
CAS:380351-29-1
分子式:C17H13Br2ClN2O
分子量：456.6
溶解度:DMF: 10 mg/ml,DMSO: 5 mg/ml,Ethanol: 1 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.¹It 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 β1 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.

1.Luo, M., Spradlin, J.N., Boike, L., et al.Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product functionCell Chem. Biol.28(4)559-566(2021)