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:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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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