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TAK-243

(別名: MLN7243)
89 Cited Publications
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Based on 89 publication(s) in Google Scholar

TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.

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  • 純度: 99.86%
  • CAS 番号: 1450833-55-2
  • 分子式: C19H20F3N5O5S2
  • 分子量:519.52
  • 保管条件:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 1 year , -20°C, 6 months
  • TAK-243 Chemical Structure
    TAK-243 構造式
  • Experimental Validation Results for TAK-243
  • Experimental Validation Results for TAK-243
  • Experimental Validation Results for TAK-243
  • Experimental Validation Results for TAK-243
  • Experimental Validation Results for TAK-243
  • Experimental Validation Results for TAK-243
  • Experimental Validation Results for TAK-243
CAS 番号: 1450833-55-2
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  • TAK-243 Chemical Structure
    TAK-243 Chemical Structure
    1/16
  • 1/16

    TAK-243 purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Feb 11;19(5):5659-5679. [Abstract]

    Customer Validation
     TAK-243/Spautin-1 groups results consistently support a positive correlation between the activity of HSP90, ubiquitination, and proteasome system with the disassembly of NSGs.

  • 1/16

    TAK-243 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2025 Feb 7;15(2):363-381. [Abstract]

    Customer Validation
     Left: immunoblot analysis assessing JAK1 expression in Myc-CaP cells that received knockout of Jak1 (Jak1 KO). Cells receiving nontargeting sgRNA were used as control. Right: surface expression of MHC-I measured by flow cytometry in the indicated cells treated with or without 50 nmol/L TAK-243 and stimulated with or without IFN-γ. Data were acquired from technical triplicates, representative of two independent experiments.

  • 1/16

    TAK-243 purchased from MedChemExpress. Usage Cited in: Nature. 2023 Jun;618(7964):394-401. [Abstract]

    Customer Validation
     The E1 inhibitor decreased the flux of ER-phagy in mCherry-GFP-FAM134B-WT cells induced with Torin 1. ER-phagy flux was quantified as the ratio between mCherry+/GFP– and mCherry+/GFP+ puncta, quantified using CQ1 software. Data are means ± s.d. of n = 5 independent experiments in which the number of cells per condition were: (DMSO) 837 basal, 1072 BafA1, 1038 Torin1, 966 BafA1+Torin1. Number of cells (10 µM TAK243): 729 basal, 1174 BafA1, 1060 Torin1, 1121 Torin1+BafA1

  • 1/16

    TAK-243 purchased from MedChemExpress. Usage Cited in: Nature. 2023 Jun;618(7964):394-401. [Abstract]

    Customer Validation
     Cells were treated with DMSO (control) or 10 µM TAK243 for 1, 2 and 4 h before TUBE-2 pulldown assays. Endogenous ubiquitination of FAM134B was detected by western blot (n = 1 experiment). The results showed that TAK243, a potent inhibitor of the ubiquitin (Ub)-activating enzyme, abolished endogenous FAM134B ubiquitination.

  • 1/16

    TAK-243 purchased from MedChemExpress. Usage Cited in: Nature. 2023 Jun;618(7964):394-401. [Abstract]

    Customer Validation
     Cycloheximide (50 µg/mL) chase for 0–6 h in HeLa cells with or without 10 µM TAK243. Detergent-soluble extracts were analysed by western blot with antibodies against FAM134B, UbP4D1 and vinculin.

  • 1/16

    TAK-243 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Jul 15;14(1):4227. [Abstract]

    Customer Validation
     Ubiquitination inhibitor TAK-243 (100 nM; 24 h) stabilizes exogenous Flag-C99 but not C83-V5 in HEK293A cells transfected with either empty vector control (pcDNA3.1) or JR-CSF.

  • 1/16

    TAK-243 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2020 Jul 16;79(2):320-331.e9. [Abstract]

    Customer Validation
     Purified BAG6-ABCG2-F208S complex was added into DMSO- or TAK-243 (MLN7243)-treated RRL and incubated at 30 ℃ for indicated times. Reactions were stopped and directly analyzed by immunoblotting for ABCG2-F208S.

  • TAK-243