MLN 4924

Name: MLN 4924
Brand: Tocris Bioscience
SKU: 6499

Tocris Bioscience, part of Bio-Techne | Catalog # 6499

Citations (37)

COA / SDS

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

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Technical Data
Citations

Product Description
Product Specifications
Solubility
Preparing Stock Solutions
Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

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

Alternative Names

Pevonedistat,TAK-924

View all NEDD8 Activating Enzyme (E1) Inhibitors »

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

Molecular Weight

443.52

Formula

C₂₁H₂₅N₅O₄S

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

	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 all 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

Calculators

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Background References

References are publications that support the biological activity of the 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