EN450

• Description :

  EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism[1].

• CAS Number :

  [793719-01-4]

• UNSPSC :

  12352005

• Hazard Statement :

  H301, H311, H331, H341

• Target :

  E1/E2/E3 Enzyme; Molecular Glues; NF-κB

• Type :

  Reference compound

• Related Pathways :

  Metabolic Enzyme/Protease; NF-κB; PROTAC

• Applications :

  Cancer-programmed cell death

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/en450.html

• Concentration :

  10mM

• Purity :

  98.59

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  O=C(NC1=CC(S(=O)(N(C)C)=O)=CC=C1Cl)C=C

• Molecular Formula :

  C11H13ClN2O3S

• Molecular Weight :

  288.76

• Precautions :

  H301, H311, H331, H341

• References & Citations :

  [1]King EA, et al. Chemoproteomics-enabled discovery of a covalent molecular glue degrader targeting NF-κB. Cell Chem Biol. 2023 Apr 20;30 (4) :394-402.e9.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported