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Biochem/physiol Actions
Cysteine reactive UBE2D/NFKB1 molecular glue degrader; NFKB1 molecular glue degrader
EN450 is a molecular glue degraders of the oncogenic transcription factor NFKB1 that 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.
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | O=C(NC1=CC(S(=O)(N(C)C)=O)=CC=C1Cl)C=C |
| InChI key | OXFXDOLAQBMOPH-UHFFFAOYSA-N |
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¥ 1082.93
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¥ 805.47
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¥ 3254.04
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¥ 1260.99
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¥ 1310.31
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¥ 1334.26
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¥ 298.24
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