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MLN 4924

Cat. No. 6499 1 Citation Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective NEDD8 activating enzyme (NAE) inhibitor; cell permeable
Alternative Names: Pevonedistat,TAK-924
Chemical Name: [(1S,2S,4R)-4-[4-[[(1S)-2,3-Dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl sulfamic acid ester
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for MLN 4924

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.

Technical Data for MLN 4924

M. Wt 443.52
Formula C21H25N5O4S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 905579-51-3
PubChem ID 16720766
InChI Key MPUQHZXIXSTTDU-QXGSTGNESA-N
Smiles N[S](=O)(=O)OC[C@@H]1C[C@H](C[C@@H]1O)N1C=CC2=C(N[C@H]3CCC4=CC=CC=C34)N=CN=C12

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.

Solubility Data for MLN 4924

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.35 100
ethanol 44.35 100

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 will affect the solvent volumes required to prepare stock solutions.

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

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Product Datasheets for MLN 4924

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for MLN 4924

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

If you know of a relevant reference for MLN 4924, please let us know.

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Keywords: MLN 4924, MLN 4924 supplier, MLN4924, NEDD8, activating, enzymes, NAE, inhibitor, inhibitors, inhibits, neddylation, cell, permeable, Pevonedistat, TAK-924, Other, Ligases, 6499, Tocris Bioscience

1 Citation for MLN 4924

Citations are publications that use Tocris products. Selected citations for MLN 4924 include:

Bruno et al (2022) Human NLRP1 is a sensor of pathogenic coronavirus 3CL proteases in lung epithelial cells. Mol Cell 82 2385-2400.e9 PMID: 35594856

Do you know of a great paper that uses MLN 4924 from Tocris? Please let us know.

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