M22

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£187.00

SKU:: 10-5733
Zusätzliche Namen:: N-[2-(2,4-dichlorophenyl)ethyl]-1-(phenylmethyl)-4-piperidinamine|NAE-IN-M22
Physischer Zustand:: Solid
Molekulargewicht:: 363.33
Reinheit:: >98%
Lagerbedingungen:: -20[o]C
Hersteller:: Focus Biomolecules
CAS Number:: 864420-54-2
Immunogen:: Neddylation
Weitere Details:: 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 uM). It has been shown to inhibit tumor growth in a mouse xenograft model (at 60 mg/kg).2