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Pevonedistat

(Synonyms: MLN4924)
226 Cited Publications
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Based on 226 publication(s) in Google Scholar

Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM. Pevonedistat induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat suppresses the growth of human tumour xenografts in mice.

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  • Reinheit: 99.55%
  • CAS. Nr.: 905579-51-3
  • Formel: C21H25N5O4S
  • Molecular Weight:443.52
  • Speicherung:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 2 years , -20°C, 1 year
  • Pevonedistat Chemical Structure
    Pevonedistat Chemical Structure
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
  • Experimental Validation Results for Pevonedistat
CAS. Nr.: 905579-51-3
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  • Pevonedistat Chemical Structure
    Pevonedistat Chemical Structure
    1/16
  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jan 15;9(1):18. [Abstract]

    Customer Validation
     MLN4924 (0.1-0.5 μM; 12 h) remarkably inhibits the neddylation of Cullin1 in splenocytes of MRL/lpr mice.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jan 15;9(1):18. [Abstract]

    Customer Validation
     MLN4924 disrupts the ubiquitination-mediated degradation pathway of Bim in DN T cells, thereby promoting Bim accumulation.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Jan 15;9(1):18. [Abstract]

    Customer Validation
     MLN4924-mediated neddylation inhibition promotes DN T cell apoptosis while increasing Bim and cleaved-caspase 3 protein levels.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2024 Jan 6:34:366-380. [Abstract]

    Customer Validation
     MLN4924 (50-200 nM) can decrease neddylation in RAW264.7 macrophages.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2024 Jan 6:34:366-380. [Abstract]

    Customer Validation
     After overnight culture, RAW264.7 macrophages were subjected to treatment with MLN4924 at concentrations of 0, 0.05, 0.1, and 0.2 μM for 12 h.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Nature. 2020 Dec;588(7836):164-168. [Abstract]

    Customer Validation
     Immunoblots of BCL6 levels in SuDHL4Cas9 cells treated with DMSO, 10 μM MLN7243 (ubiquitin activating enzyme inhibitor), 10 μM MG132 (26S proteasome inhibitor), 10 μM Chloroquine (lysosomal inhibitor), or 5 μM MLN4924 (neddylation inhibitor) for 15 minutes, then, for indicated samples, 1 μM BI-3802 was added and 35 minutes later, 10 μM BI-3812 was added for the final 10 minutes, resulting in a total of 1 hour treatment with MLN7243, MG132, Chloroquine, and MLN4924, 45 minutes of BI-3802, and 10

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Cell Res. 2021 Mar;31(3):291-311. [Abstract]

    Customer Validation
     MLN4924 (1 μM; 12 h). Immunoblot of WCL from MCF-7 cells transfected with Myc-PTEN (a), or tissues of WT or NEDP1 KO mice (b), or NEDP1-deleted MCF-7 cells (c).

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2019 May;4(5):813-825. [Abstract]

    Customer Validation
     293T cells are treated with MLN4924 and then co-transfected with PSGL-1 and Vpu or an empty vector. One day after the transfection, the cells are treated with CHX and collected at the indicated time points. The cell lysates are analysed by western blotting.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2019 May;4(5):813-825. [Abstract]

    Customer Validation
     293T cells are treated with MLN4924 at the indicated concentrations 24 h before the cells are transfected with plasmids expressing PSGL-1 and Vpu. Two days after transfection, the cells are harvested and analysed by western blotting. Empty vector (–) was used as a negative control for the Vpu- or PSGL-1-expressing vectors.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Nat Plants. 2019 Jan;5(1):34-40.  [Abstract]

    Customer Validation
     Western analysis of LHCSR1 and LHCSR3 protein expression in the treatment of MLN4924 with different concentrations.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Lab Invest. 2019 Apr;99(4):528-538. [Abstract]

    Customer Validation
     Western blot analysis of p65 phosphorylation in synovial cells induced by 100 ng/ml IL-17A with or without 100 nM MLN4924 pretreatment.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2019 Jun 1;316(6):L1070-L1080. [Abstract]

    Customer Validation
     Immunoblotting analysis of degradation of IκBα, and levels of p-p65 (also known as RELA) and the NEDD8–Cullin compared with β-actin and total p65 in cell lysates from pulmonary epithelial cells stimulated with rmIL-17A (50 ng/ml) for 15 min after preincubation with the indicated concentration of MLN4924 (MLN) or DMSO for 0.5 h.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2019 Jun 1;316(6):L1070-L1080. [Abstract]

    Customer Validation
     Immunoblotting analysis of p-p38, JNK, and ERK compared with total p38, JNK, and ERK in cell lysates from pulmonary epithelial cells stimulated as above.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2019 Jan 15;508(3):986-990.  [Abstract]

    Customer Validation
     MLN4924 antagonizes the suppressive effects of PTX on cytoskeletal organization in HO8910 and OVA-W cells. (A, C) After treatment with PTX and/or MLN4924 for 48 h, HO8910 and OVA-W cells are stained for α-tubulin and analyzed for intracellular distribution by confocal microscopy. Overlay of blue (nuclei) and red (a-tubulin) channels is shown. (B, D) Levels of α-tubulin protein are further confirmed by western blotting with b-actin as the loading control.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Sep 18;9(1):3801. [Abstract]

    Customer Validation
     Trophozoites (3D7) are subjected to the indicated treatment for 6 h before analysis of ubiquitinated proteins. Samples treated with MLN4924 are incubated for an additional 3 h prior to DHA treatment. Blots are representative of 3-4 independent experiments.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Elife. 2018 Aug 1;7:e38430. [Abstract]

    Customer Validation
     Kelly cells are treated with increasing concentrations of Thal and co-treated with 5 μM Bortezonib, 5 μM MLN4924, 0.5 μM MLN7243, or DMSO as a control. Following 24 h incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Int J Med Sci. 2018 Apr 3;15(7):674-681. [Abstract]

    Customer Validation
     NB4 cells are treated with MLN4924 (0, 20, 40 and 80 nM) for 0, 24, 48 and 72 hours, and the protein levels of cullin1 are detected by western blotting, with β-actin used as loading control.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Cancer Chemother Pharmacol. 2018 Jun;81(6):1083-1093. [Abstract]

    Customer Validation
     786-0 and ACHN cells are treated with MLN4924 (0.5 μM or 1 μM).γ-H2AX is detected by immunoblotting analysis.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Dec;22(23):8273-8280. [Abstract]

    Customer Validation
     AGS cells are transfected with increased dose of Flag-FBXW8 for 30 hours, 2 μM MLN4924 are added where indicate 4 hours before harvested. Western blot assay is performed with indicated antibodies.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Dec;22(23):8273-8280. [Abstract]

    Customer Validation
     MRFAP1 KO AGS cells are treated with or without 2 μM MLN4924 for 24 hours, cells are harvested and subjected to Western blot with indicated antibodies.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Dec;22(23):8273-8280. [Abstract]

    Customer Validation
     AGS cells are transfected with Flag-MRFAP1 for 30 hours and treated with or with 2 μM MLN4924 for additional 4 hours, cells are harvested and subjected to immunoprecipitation with Flag M2 beads and then detected with Western blot.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Sep 23;8(49):86395-86409. [Abstract]

    Customer Validation
     Immunofluorescence results, showing that ROC1, DCAF1, DDB1, and TET1 knockdown, and treatment with MLN4924 leads to the reduction of 5hmC levels in A2780 cells. A2780 cells transfected with siNC, siROC1, siDCAF1, siDDB1 or siTET1 and treatment with MLN4924 are subjected to immunofluorescence analysis with antibodies to the indicated protein.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Oct 12;8(57):97178-97186. [Abstract]

    Customer Validation
     After 4 hours 1 µM MLN4924 treatment, lysates from 293T cells stably expressing either Flag or Flag-FBXW8 are immunoprecipitated with anti-FLAG M2 resin. Bound proteins are eluted with FLAG peptide, and all separated cell lysate components are resolved on 10% SDS-PAGE gel, stained by Coomassie Brilliant or subjected to immunoblotting with the indicated antibodies.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Elife. 2016 Apr 11;5:e14087. [Abstract]

    Customer Validation
     Fbxo21-/- RAW264.7 cells are transfected with indicated amounts (0, 1 or 5 μg) Fbxo21-Myc and equal amounts of K29O-Ub-HA vectors for 48 hr, and then infected with VSV (MOI = 1) or HSV-1 (MOI = 5) for 2 hr in the presence or absence of MLN-4924 (10 nM). Then polyubiquitinated ASK1 is examined by immunoblot (IB) against HA after immuneprecipitations (IP).

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Technol Cancer Res Treat. 2016 Aug;15(4):527-34. [Abstract]

    Customer Validation
     MLN4924 induces accumulation of SCF E3 ligase substrates. Subconfluent cells are treated with MLN4924 (50 nM) or radiation (6 Gy) alone or in combination for 24 hours, followed by immunoblotting (IB) analysis using indicated antibodies.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Jun 14;7(24):35643-35654. [Abstract]

    Customer Validation
     MLN4924 induces apoptosis is caspase dependent. BMDCs are cultured with MLN4924. Total cellular protein extracts are prepared and subjected to immunoblotting by using A. anti-PARP, anti-caspase-3, anti-caspase-7 antibodies and B. anti-cleaved PARP, anti-cleaved-caspase-3, anti-cleaved-caspase-7 antibodies. C. Caspase-3 activity is examined by caspase activity kit. D. Immunoblotting analysis is performed for erk, p-erk, cyclin D1 and cyclin D3 expression.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Oct 4;7(40):66087-66099. [Abstract]

    Customer Validation
     MLN4924 increases the stability of RORα. MLN4924 increases the half-life of RORα. U2OS cells are transiently transfected with plasmids expressing the Flag-RORα. At 24 h after transfection, MLN4924 (1 μM) or DMSO are added into respective cell culture media. 24 h later, cells are treated with Cycloheximide (CHX) for 0, 3, 6, 4, 9 and 12 h. Equal amounts of whole cell lysates are analyzed by Western blot with a Flag antibody (M2). Actin is used as an internal control.

  • 1/16

    Pevonedistat purchased from MedChemExpress. Usage Cited in: Ann Hematol. 2014 Sep;93(9):1499-508. [Abstract]

    Customer Validation
     MLN4924-induced p21 high expression eliminates the cell cycle promotion effect of BM-MSCs on Reh cells. a Western blot analysis of p21, skp2, and bax expression in Reh cells treated by different concentration of MLN4924. b Under the treatment of 25 nM IDA, western blot analysis of p21 and skp2 expressions in Reh cells cultured with or without BM-MSCs in the presence of different concentrations of MLN4924 (0, 300, 700 nM). c Under the treatment of 250 nM VP16, western blot analysis of p21 and skp

  • Pevonedistat