| Identification | Back Directory | [Name]
N-[2-Chloro-5-[(dimethylamino)sulfonyl]phenyl]-2-propenamide | [CAS]
793719-01-4 | [Synonyms]
EN450
N-[2-Chloro-5-[(dimethylamino)sulfonyl]phenyl]-2-propenamide | [Molecular Formula]
C11H13ClN2O3S | [MOL File]
793719-01-4.mol | [Molecular Weight]
288.75 |
| Chemical Properties | Back Directory | [density ]
1.364±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
12.16±0.70(Predicted) | [color ]
White to off-white | [InChIKey]
OXFXDOLAQBMOPH-UHFFFAOYSA-N | [SMILES]
O=C(NC1=CC(S(=O)(N(C)C)=O)=CC=C1Cl)C=C |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
EN450 is a molecular glue degraders of the oncogenic transcription factor NFKB1 th at induces ternary complex formation between ubiquitin-conjugating enzyme E2D1 (UBE2D1) and NFKB1. EN450 covalently modifies an allosteric C111 in UBE2D1 and significantly reduces NFKB1 p105 levels. It impairs leukemia cell viability in a NEDDylation and proteasome-dependent manner at 50 μM. | [References]
[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. DOI:10.1016/j.chembiol.2023.02.008 |
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