EN450

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].

Product Specifications

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.