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TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
| Molecular Weight | 519.52 |
| CAS Number | 1450833-55-2 |
| Solubility (25°C) | DMSO 50 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
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. |
| Iberdomide
Iberdomide (CC-220) is an orally effective cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 for cereblon binding affinity of approximately 150 nM. Iberdomide (CC-220) binds CRBN with higher affinity than lenalidomide and pomalidomide and has enhanced degradation of IKZF1 and IKZF3 with enhanced degradation. |
| Ginkgolic Acid
Ginkgolic Acid is a inhibits SUMOylation by binding E1. |
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