EN219

• Target :

  E1/E2/E3 Enzyme|||Others

• Related Pathways :

  Others|||Ubiquitination

• Bioactivity :

  EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114 and binds specifically to cysteine 8 (C8) within its intrinsically disordered region, exhibiting an IC50 of 470 nM. EN219 inhibits RNF114-induced autoubiquitination and p21 ubiquitination in cell-free assays at 50 ?M. At 1 ?M, EN219 interacts with multiple proteins including the tubulin ?1 chain (TUBB1), heat shock protein 60 (Hsp60/HspD1), and histone H3.1 (HIST1H3A) in 231MFP breast cancer cells. Furthermore, EN219 has been linked to the bromodomain inhibitor (+) -JQ1 for the creation of a PROTAC capable of degrading BRD4 in 231MFP cells.

• Smiles :

  O=C(N1N=C(C=2C=CC(Br)=CC2)CC1C3=CC=C(Br)C=C3)CCl

• Molecular Formula :

  C17H13Br2ClN2O

• Molecular Weight :

  456.56

• Shipping Conditions :

  Cool pack

• Storage Temperature :

  -20°C

• CAS Number :

  380351-29-1