纯度:>98% by TLC;NMR (Conforms)
分子式:C20H24Cl2N2
分子量:363.33
溶剂:DMSO (40 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):NEDD8 activating enzyme inhibitor
Function / Pharmacology: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