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In vitro: Lenalidomide and pomalidomide, targeting cereblon, are immunomodulatory drugs that are clinically effective in the treatment of cancer, including newly diagnosed and relapsed multiple myeloma. Iberdomide contains a glutarimide ring that binds in the try-tryptophan pocket of cereblon and an isoindolinone ring that can interact with both cereblon and substrates. Treatment with Iberdomide results in the loss of Ikaros and Aiolos protein levels with EC50s of 1 nM and 0.5 nM. In vivo: Iberdomide (CC-220) is currently in phase 2 clinical trials for the treatment of systematic lupus erythematosus (SLE) and phase 1b/2a clinical trials for relapsed and refractory multiple myeloma (MM).
| Molecular Weight | 449.5 |
| Formula | C25H27N3O5 |
| CAS Number | 1323403-33-3 |
| Solubility (25°C) | DMSO >100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related E1/E2/E3 Enzyme Products |
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NSC697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A. |
| PYR-41
PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2. |
| CC0651
CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme and inhibited the ubiquitination of p27Kip1 with IC50 value of 1.72 μM. |
| Ginkgolic Acid
Ginkgolic Acid is a inhibits SUMOylation by binding E1. |
| Heclin
Heclin is a hECT E3 ubiquitin ligase inhibitor. |
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