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

Subasumstat  (Synonyms: TAK-981)

製品番号: HY-111789 純度: 98.38%
COA 取扱説明書 Technical Support

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

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1858276-04-6

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 254 在庫あり
Solution
10 mM * 1 mL in DMSO USD 254 在庫あり
Solid
1 mg $95 在庫あり
5 mg $200 在庫あり
10 mg $310 在庫あり
25 mg $593 在庫あり
50 mg $950 在庫あり
100 mg $1650 在庫あり
200 mg $2640 在庫あり
500 mg $4950 在庫あり
1 g   お問い合わせ  
5 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

カスタマーレビュー

Based on 33 publication(s) in Google Scholar

Other Forms of Subasumstat:

Top Publications Citing Use of Products
WB
In Vivo Efficacy Study
Cell Migration/Invasion Assay
RT-PCR
Cell Proliferation/Viability Assay

    Subasumstat purchased from MedChemExpress. Usage Cited in: iScience. 2024 Oct 11;27(11):111133.  [Abstract]

    Leader and follower cells treated with indicated doses of TAK-981 for 72 h were evaluated for YAP and TAZ.

    Subasumstat purchased from MedChemExpress. Usage Cited in: iScience. 2024 Oct 11;27(11):111133.  [Abstract]

    Mice were treated with vehicle or 25 mg/kg TAK-981 thrice weekly. Bright-field images of tumors isolated from vehicle- and TAK-981-treated mice were captured.

    Subasumstat purchased from MedChemExpress. Usage Cited in: iScience. 2024 Oct 11;27(11):111133.  [Abstract]

    Spheroids generated with leader cells, follower cells, or mixes of 90% follower cells and 10% leader cells (L:F, 1:9) treated with either DMSO or 250 nM TAK-981 (72 h) were evaluated for invasive area with quantification of invasive area.

    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 Dec;7(12):2101-2113.  [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.
    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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].

    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 EC50
    0.063 3
    Compound: TAK-981
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    [PMID: 33631934]
    HCT-116 EC50
    0.063 3
    Compound: TAK-981
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    [PMID: 33631934]
    OCI-Ly10 EC50
    0.004 3
    Compound: TAK-981
    Cytotoxicity against human OCI-LY10 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    Cytotoxicity against human OCI-LY10 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    [PMID: 33631934]
    OCI-Ly10 EC50
    0.004 3
    Compound: TAK-981
    Cytotoxicity against human OCI-LY10 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    Cytotoxicity against human OCI-LY10 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    [PMID: 33631934]
    HCT-116 EC50
    0.063 3
    Compound: TAK-981
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    [PMID: 33631934]
    OCI-Ly10 EC50
    0.004 3
    Compound: TAK-981
    Cytotoxicity against human OCI-LY10 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    Cytotoxicity against human OCI-LY10 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
    [PMID: 33631934]
    体外実験

    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.

    体内実験

    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.

    臨床実験
    分子量

    578.10

    分子式

    C25H28ClN5O5S2

    CAS 番号
    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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (172.98 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 1.7298 mL 8.6490 mL 17.2980 mL
    5 mM 0.3460 mL 1.7298 mL 3.4596 mL
    10 mM 0.1730 mL 0.8649 mL 1.7298 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
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始)

    C1

    ×
    体積 (開始)

    V1

    =
    濃度 (終了)

    C2

    ×
    体積 (終了)

    V2

    体内:

    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: ≥ 5 mg/mL (8.65 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

      Solubility: ≥ 5 mg/mL (8.65 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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.
    純度とドキュメンテーション

    純度: 98.53%

    参考文献

    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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
    × = ×
    C1   V1   C2   V2
    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.

    最近チェックした製品:

    オンラインお問い合わせ

    Your information is safe with us. * Required Fields.

    製品名

     

    カスタマ需要量 *

    お名前 *

     

    タイトル

    メールアドレス *

     

    電話番号 *

    デパートメント

     

    組纖名 *

    市区町村

    都道府県

    国或いは地域 *

         

    必ず会社名を記載ください。個人への返信は行いません。

    備考

    バルクお問い合わせ

    Inquiry Information

    製品名:
    Subasumstat
    製品番号:
    HY-111789
    数量:
    MCE 日本正規代理店: