MLN 4924

Catalog # Availability Size / Price Qty
6499/50
6499/10
MLN 4924 | CAS No. 905579-51-3 | NEDD8 Activating Enzyme (E1) Inhibitors
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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%

Product Details
Citations (1)
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Biological Activity

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

M.Wt:
443.52
Formula:
C21H25N5O4S
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
905579-51-3

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.

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Citation for MLN 4924

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