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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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 will affect the solvent volumes required to prepare stock solutions.
|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|
References are publications that support the biological activity of the product.
Baek et al (2020) NEDD8 nucleates a multivalent cullin-RING-UBE2D ubiquitin ligation assembly. Nature 578 461 PMID: 32051583
Soucy et al (2009) An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature 458 732 PMID: 19360080
Brownell et al (2010) Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ. Mol.Cell 37 102 PMID: 20129059
Zhou et al (2016) Blockage of neddylation modification stimulates tumor sphere formation in vitro and stem cell differentiation and wound healing in vivo. Proc.Natl.Acad.Sci.USA 113 E2935 PMID: 27162365
Hyer et al (2018) A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. Nat.Med. 24 186 PMID: 29334375
Tong et al (2017) MLN4924 (Pevonedistat), a protein neddylation inhibitor, suppresses proliferation and migration of human clear cell renal cell carcinoma. Sci.Rep. 7 5599 PMID: 28717191
Wolenski et al (2015) The NAE inhibitor pevonedistat (MLN4924) synergizes with TNF-α to activate apoptosis. Cell Death Discov. 1 doi: 10.1038 PMID: 27551465
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Keywords: MLN 4924, MLN 4924 supplier, MLN4924, NEDD8, activating, enzymes, NAE, inhibitor, inhibitors, inhibits, neddylation, cell, permeable, Other, Ligases, 6499, Tocris Bioscience
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