A selective inhibitor of NEDD8-activating enzyme
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MLN4924

Item No. 15217

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
sulfamic acid, [(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 ester
CAS Number
905579-51-3
Synonyms
  • Pevonedistat
Molecular Formula
C21H25N5O4S
Formula Weight
443.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 10 mg/ml
λmax
213, 279 nm
SMILES
O[C@H]([C@H](COS(N)(=O)=O)C1)C[C@@H]1N2C=CC3=C(N[C@@H]4C(C=CC=C5)=C5CC4)N=CN=C23
InChi Code
InChI=1S/C21H25N5O4S/c22-31(28,29)30-11-14-9-15(10-19(14)27)26-8-7-17-20(23-12-24-21(17)26)25-18-6-5-13-3-1-2-4-16(13)18/h1-4,7-8,12,14-15,18-19,27H,5-6,9-11H2,(H2,22,28,29)(H,23,24,25)/t14-,15+,18-,19-/m0/s1
InChi Key
MPUQHZXIXSTTDU-QXGSTGNESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $58

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    5 mg

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    10 mg

    $201

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    Cayman Chemical
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    Product Description

    MLN4924 is an analog of adenosine 5’-monophosphate that selectively inhibits NAE (IC50 = 4.7 nM).1 At much higher concentrations, MLN4924 inhibits the related enzymes ubiquitin-activating enzyme (UAE) and SUMO-activating enzyme (SAE) with IC50 values of 1.5 and 8.2 μM, respectively.1 At 0.3 μM, MLN4924 has been shown to disrupt CRL-mediated protein turnover leading to apoptosis in HCT116 cells by deregulating S-phase DNA synthesis.1 In vivo, 30-60 mg/kg MLN4924 dose-dependently suppresses the growth of human tumor xenografts in mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Soucy, T.A., Smith, P.G., Milhollen, M.A., et al. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature 458(7239), 732-736 (2009).

    Product Citations

    Law, R.P., Nunes, J., Chung, C.-W., et al. Discovery and characterisation of highly cooperative FAK-degrading PROTACs. Angew. Chem. Int. Ed. Engl. 60(43), 23327-23334 (2021).