2. Metabolic Enzyme/Protease NF-κB Apoptosis
  3. E1/E2/E3 Enzyme NF-κB Apoptosis
  4. TAK-243

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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CAS No. : 1450833-55-2

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Customer Review

Based on 83 publication(s) in Google Scholar

Other Forms of TAK-243:

TAK-243 Related Antibodies

Top Publications Citing Use of Products

83 Publications Citing Use of MCE TAK-243

RT-PCR
IHC
WB

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

    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.

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

    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.

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

    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

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

    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.

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

    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.

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

    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.

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

    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.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2].

    IC50 & Target

    IC50: 1 nM (UBA1)[1]
    In Vitro

    TAK-243 shows anti-proliferative effect on a panel of cell lines derived from hematologic and solid tumors with variable EC50 values that ranged from 0.006 μM to 1.31 μM[1].
    ? TAK-243 reduces growth and viability of human AML cell lines (OCI-AML2, TEX, U937 and NB4) in a concentration- and time-dependent manner with IC50s ranging from 15-40 nM after treatment for 48 hours[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    TAK-243 Related Antibodies
    In Vivo

    TAK-243 significantly delays tumor growth in mice (T/C=0.02) with no toxicity as evidenced by no changes in mouse body weight, serum chemistry, or organ histology. TAK-243 reduces primary AML tumor burden in both tested samples without toxicity[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    519.52

    Formula

    C19H20F3N5O5S2
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=S(OC[C@@H]1[C@@H](O)[C@@H](O)[C@H](NC2=CC=NC3=CC(C4=CC=CC(SC(F)(F)F)=C4)=NN23)C1)(N)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (96.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9249 mL 9.6243 mL 19.2485 mL
    5 mM 0.3850 mL 1.9249 mL 3.8497 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
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    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.86%

    SDS (396 KB)

    COA (261 KB) HNMR (146 KB) RP-HPLC (163 KB) LCMS (108 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Normal keratinocytes (normal human keratinocytes (NHK) and recessive dystrophic epidermolysis bullosa keratinocytes (RDEBK)) and cSCC cell lines are seeded into 96 well plates and live cell number and cell death are analysed with an IncuCyte ZOOM real-time imager using the CellTox Green Cytotoxicity Assay. Relative EC50 values are determined using GraphPad Prism. For clonogenic assays cells are seeded into six well plates. Inhibitors (e.g., TAK-243; 0.01, 0.1, 1, and 10 μM) are added for the indicated times and then cells are maintained in drug-free medium for up to 2 weeks to allow colony formation. Colonies are fixed in 10% methanol, 10% acetic acid and stained with crystal violet[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    The preclinical efficacy and toxicity of TAK-243 are assessed in mouse models of AML. OCI-AML2 cells are injected subcutaneously (sc) into SCID mice, and when tumors are palpable, mice are treated with TAK-243 (20 mg/kg sc twice weekly). As an additional model, primary AML cells from 2 patients are injected into the femurs of NOD-SCID mice. Two weeks after injection, mice are treated with TAK-243 (20 mg/kg sc twice weekly). After 3 weeks of treatment, mice ae sacrificed, and AML engraftment in the non-injected femur is measured by flow cytometry[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9249 mL 9.6243 mL 19.2485 mL 48.1213 mL
    5 mM 0.3850 mL 1.9249 mL 3.8497 mL 9.6243 mL
    10 mM 0.1925 mL 0.9624 mL 1.9249 mL 4.8121 mL
    15 mM 0.1283 mL 0.6416 mL 1.2832 mL 3.2081 mL
    20 mM 0.0962 mL 0.4812 mL 0.9624 mL 2.4061 mL
    25 mM 0.0770 mL 0.3850 mL 0.7699 mL 1.9249 mL
    30 mM 0.0642 mL 0.3208 mL 0.6416 mL 1.6040 mL
    40 mM 0.0481 mL 0.2406 mL 0.4812 mL 1.2030 mL
    50 mM 0.0385 mL 0.1925 mL 0.3850 mL 0.9624 mL
    60 mM 0.0321 mL 0.1604 mL 0.3208 mL 0.8020 mL
    80 mM 0.0241 mL 0.1203 mL 0.2406 mL 0.6015 mL
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    TAK-243 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    TAK-2431450833-55-2MLN7243TAK243TAK 243MLN 7243MLN-7243E1/E2/E3 EnzymeNF-κBApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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