EN450
CAS No. : 793719-01-4
| Size | Price | Stock |
|---|---|---|
| 50mg | $750 | In-stock |
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| Cat. No. : | HY-49444 |
| M.Wt: | 288.76 |
| Formula: | C11H13ClN2O3S |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
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].
In Vitro:EN450 (50 μM; 24 h) significantly inhibits the proliferation of HAP1 leukemia cancer cells and HEK293T cells, and significantly reduces the levels of the p105 and p50 subunits of the oncogenic transcription factor NFκB1[1].
EN450 (50 μM; 1 h) enhances the ubiquitination of NFκB1 mediated by UBE2D1 in the presence of the full CUL4A/RBX1/NEDD8 complex[1].
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