Potent and selective NEDD8 activating enzyme (NAE) inhibitor; cell permeable
MLN 4924 (Tak 924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50 = 4.7 nM). MLN 4924 exhibits selectivity over closely related enzymes UAE, UBA6, SAE, and ATG7 (IC50 = 1.5, 1.8, 8.2, and >10 μM, respectively), and displays minimal activity at adenosine receptors and a panel of 12 cellular kinases. MLN 4924 exhibits cyotoxicity in several human tumor-derived cell lines and causes liver damage in SD rats, when given with TNF-α. It blocks the NEDD8 pathway causing DNA damage in mice bearing HCT-116 xenografts. Cell permeable.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-124360 |
| Réf. fabricant | 18779236 |
| Nom chimique ou matériau | [(1 S,2 S,4 R)-4-[4-[[(1 S)-2,3-Dihydro-1 H-inden-1-yl]amino]-7 H-pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl sulfamic acid ester |
| CAS | 905579-51-3 |
| Quantité | 10 mg |
| Cible | NEDD8 Activating Enzyme E1) |
| Formule moléculaire | C<sub>21</sub>H<sub>25</sub>N<sub>5</sub>O<sub>4</sub>S |
| Pureté | 0.98 |
