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M22

CAT: 0498-bs-83460C-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0498-bs-83460C-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Background
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
Conjugation
Unconjugated
Buffer
Off-white solid
Storage Conditions
-20°C

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