MLN 4924

Key Product Details

Product 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.

Product Specifications for MLN 4924

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for MLN 4924

The following data is based on the product molecular weight 443.52.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.25 mL	11.27 mL	22.55 mL
5 mM	0.45 mL	2.25 mL	4.51 mL
10 mM	0.23 mL	1.13 mL	2.25 mL
50 mM	0.05 mL	0.23 mL	0.45 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 28 publications citing the usage of this product.

• Tong MLN4924 (Pevonedistat), a protein neddylation inhibitor, suppresses proliferation and migration of human clear cell renal cell carcinoma. Sci.Rep. 2017 PMID: 28717191
• Wolenski The NAE inhibitor pevonedistat (MLN4924) synergizes with TNF-α to activate apoptosis. Cell Death Discov. 2015 PMID: 27551465
• Hyer A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. Nat.Med. 2018 PMID: 29334375
• Zhou Blockage of neddylation modification stimulates tumor sphere formation in vitro and stem cell differentiation and wound healing in vivo. Proc.Natl.Acad.Sci.USA 2016 PMID: 27162365
• Brownell Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ. Mol.Cell 2010 PMID: 20129059
• Soucy An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature 2009 PMID: 19360080
• Baek NEDD8 nucleates a multivalent cullin-RING-UBE2D ubiquitin ligation assembly. Nature 2020 PMID: 32051583

Product Documents for MLN 4924