M22 | NEDD8 activating enzyme inhibitor
Available Options
| Size | Price | Quantity | |
|---|---|---|---|
| 5mg | $110.00 | ||
| 25mg | $400.00 |
Protein neddylation is a post-translational modification which transfers the ubiquitin-like protein NEDD8 to a lysine residue of the target substrate through a three-step enzymatic cascade and has been considered as a viable target for the development of new therapeutics for cancer.1 M22 (CAS 864420-54-2) is an inhibitor of NEDD8 activating enzyme (NAE) which was discovered by virtual screening of a small molecule library (50,000 compounds) against the active site of NAE.2 M22 is selective and reversible and inhibits NEDDylation of ubiquitin-conjugating enzyme 12 (UBC12) in a cell-free assay employing recombinant human NAE. It selectively inhibits NEDDylation over SUMOylation and ubiquitination in A549 cells and inhibits their growth (GI50 = 5.5 µM). It has been shown to inhibit tumor growth in a mouse xenograft model (at 60 mg/kg).2
References/Citations:
- Zhong et al. (2012), Discovery of a natural product inhibitor targeting protein neddylation by structure-based virtual screening; Biochimie, 94 2457
- Lu et al. (2016), Discovery of a novel NEDD8 activating enzyme inhibitor with piperidin-4-amine scaffold by structure-based virtual screening; ACS Chem. Biol., 11 1901
C20H24Cl2N2
>98% TLC
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
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Protein neddylation is a post-translational modification which transfers the ubiquitin-like protein NEDD8 to a lysine residue of the target substrate through a three-step enzymatic cascade and has been considered as a viable target for the development of new therapeutics for cancer.1 M22 (CAS 864420-54-2) is an inhibitor of NEDD8 activating enzyme (NAE) which was discovered by virtual screening of a small molecule library (50,000 compounds) against the active site of NAE.2 M22 is selective and reversible and inhibits NEDDylation of ubiquitin-conjugating enzyme 12 (UBC12) in a cell-free assay employing recombinant human NAE. It selectively inhibits NEDDylation over SUMOylation and ubiquitination in A549 cells and inhibits their growth (GI50 = 5.5 µM). It has been shown to inhibit tumor growth in a mouse xenograft model (at 60 mg/kg).2
References/Citations:
- Zhong et al. (2012), Discovery of a natural product inhibitor targeting protein neddylation by structure-based virtual screening; Biochimie, 94 2457
- Lu et al. (2016), Discovery of a novel NEDD8 activating enzyme inhibitor with piperidin-4-amine scaffold by structure-based virtual screening; ACS Chem. Biol., 11 1901
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