Tocris Bioscience™ MLN 4924

Potent and selective NEDD8 activating enzyme (NAE) inhibitor; cell permeable

Brand:  Tocris Bioscience™ 6499/10

Product Code. 18779236

Description

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.

Specifications

• Chemical Name or Material: [(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
• Quantity: 10 mg
• Molecular Formula: C₂₁H₂₅N₅O₄S

• CAS: 905579-51-3
• Target: NEDD8 Activating Enzyme E1)
• Purity: 0.98