EN219

EN219

CAT N°: 33957
Price:

From 49.00 41.65

EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.{60543} 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 ?1 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.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 1-[3,5-bis(4-bromophenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-chloro-ethanone
  • Correlated keywords
    • EN-219 RNF-114 RNF114C8 p-21 TUBB-1 Hsp-60 D1 HspD-1 231-MFP BRD-4 HIST1-H3A
  • Product Overview:
    EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.{60543} 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 ?1 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.

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