2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. Subasumstat

Subasumstat  (Synonyms: TAK-981)

Cat. No.: HY-111789 Purity: 98.56%
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Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.

For research use only. We do not sell to patients.

Subasumstat Chemical Structure

Subasumstat Chemical Structure

CAS No. : 1858276-04-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 254 In-stock
Solution
10 mM * 1 mL in DMSO USD 254 In-stock
Solid
1 mg USD 95 In-stock
5 mg USD 200 In-stock
10 mg USD 310 In-stock
25 mg USD 593 In-stock
50 mg USD 950 In-stock
100 mg USD 1650 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Subasumstat:

Subasumstat Related Antibodies

Top Publications Citing Use of Products

    Subasumstat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 21;14(2):147.  [Abstract]

    Subasumstat (TAK-981; 25 mg/kg; every 3 days for 21 days) suppresses the growth of glioblastoma in mice.

    Subasumstat purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2022 Nov 14.  [Abstract]

    Subasumstat (TAK-981) boosts NLuc expression from unintegrated HIV-1 DNA, reaching a plateau at ~75 nM. Subasumstat is added to CEM-SS Cas9 and ΔSMC5 cells infected with NL-NLuc at 0, 5, 15, 30, 75, 150, 500 and 1,000 nM concentrations, and the cells are collected for an NLuc assay after 2 dpi.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities[1][2].

    IC50 & Target

    SUMOylation[1].
    In Vitro

    Subasumstat (TAK-981) is able to increase the production of type 1 IFN, thereby increasing type 1 IFN-mediated signaling, activating innate effector cells and enhancing the antitumor innate immune responses[1].

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

    Subasumstat Related Antibodies
    In Vivo

    A single sub-cutaneous injection of Subasumstat (TAK-981) in naive Balb/c mice at the brachial lymph nodes induces activation of DCs[2].

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

    578.10

    Formula

    C25H28ClN5O5S2
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=S(OC[C@@H]1[C@@H](O)C[C@H](NC2=NC=NC=C2C(C3=CC([C@@H]4NCCC5=C4C=C(Cl)C=C5)=C(C)S3)=O)C1)(N)=O
    Shipping

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

    DMSO : ≥ 100 mg/mL (172.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7298 mL 8.6490 mL 17.2980 mL
    5 mM 0.3460 mL 1.7298 mL 3.4596 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 2.5 mg/mL (4.32 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.32 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    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: 98.56%

    COA (256 KB) HNMR (338 KB) LCMS (150 KB)

    Handling Instructions (2659 KB)
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7298 mL 8.6490 mL 17.2980 mL 43.2451 mL
    5 mM 0.3460 mL 1.7298 mL 3.4596 mL 8.6490 mL
    10 mM 0.1730 mL 0.8649 mL 1.7298 mL 4.3245 mL
    15 mM 0.1153 mL 0.5766 mL 1.1532 mL 2.8830 mL
    20 mM 0.0865 mL 0.4325 mL 0.8649 mL 2.1623 mL
    25 mM 0.0692 mL 0.3460 mL 0.6919 mL 1.7298 mL
    30 mM 0.0577 mL 0.2883 mL 0.5766 mL 1.4415 mL
    40 mM 0.0432 mL 0.2162 mL 0.4325 mL 1.0811 mL
    50 mM 0.0346 mL 0.1730 mL 0.3460 mL 0.8649 mL
    60 mM 0.0288 mL 0.1442 mL 0.2883 mL 0.7208 mL
    80 mM 0.0216 mL 0.1081 mL 0.2162 mL 0.5406 mL
    100 mM 0.0173 mL 0.0865 mL 0.1730 mL 0.4325 mL
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    Subasumstat 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:

    Subasumstat1858276-04-6TAK-981TAK981TAK 981E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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