2. Metabolic Enzyme/Protease Apoptosis
  3. E1/E2/E3 Enzyme c-Myc
  4. BI8622

BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM. BI8622 can decrease the protein expression levels of c-myc and glycolytic markers as well as immune modulatory markers after HUWE1 inhibition in triple-negative breast cancer (TNBC) cell lines. BI8622 significantly protects against cisplatin (HY-17394)-induced acute kidney injury (AKI). BI8622 significantly reduces the growth of multiple myeloma (MM) cell lines and induces cell cycle arrest. BI8622 can prevent HUWE1-dependent TTBK2 ubiquitination. BI8622 can be studied in research for various diseases including medulloblastoma, acute kidney injury, breast cancer and MM.

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CAS 番号 : 1875036-74-0

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 385 在庫あり
Solution
10 mM * 1 mL in DMSO USD 385 在庫あり
Solid
5 mg $350 在庫あり
10 mg $550 在庫あり
25 mg $972 在庫あり
50 mg $1360 在庫あり
100 mg $1900 在庫あり
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500 mg   お問い合わせ  

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Based on 4 publication(s) in Google Scholar

BI8622 関連抗体

Top Publications Citing Use of Products

    BI8622 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2020 Dec;27(12):3273-3288.  [Abstract]

    Protein expression of Myst2 in Huwe1 inhibits mESCs is analyzed by Western blot using Huwe1 inhibitor (BI8622). Indicated amounts of BI8622 is treated for 24 h to inhibit Huwe1.

    BI8622 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2020 Dec 1;130(12):6301-6316.  [Abstract]

    Immunoblot analysis of pro–caspase-1 and its subunit p20. Caspase-1 activation in NLRP3, AIM2, and NLRC4 inflammasomes is substantially reduced in BMDMs treated with BI8622 (10 μM) compared with untreated BMDMs.

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    製品説明

    BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM. BI8622 can decrease the protein expression levels of c-myc and glycolytic markers as well as immune modulatory markers after HUWE1 inhibition in triple-negative breast cancer (TNBC) cell lines. BI8622 significantly protects against cisplatin (HY-17394)-induced acute kidney injury (AKI). BI8622 significantly reduces the growth of multiple myeloma (MM) cell lines and induces cell cycle arrest. BI8622 can prevent HUWE1-dependent TTBK2 ubiquitination. BI8622 can be studied in research for various diseases including medulloblastoma, acute kidney injury, breast cancer and MM[1][2][3][4][5].

    IC50 & Target

    IC50: 3.1 μM (HUWE1)[1]
    体外実験

    BI8622 induces HUWE1 ectopically expresses to abolish ubiquitination of MCL1 with an IC50 value of 6.8 μM in HeLa cells[1].
    BI8622 (10 μM, 1-4 days) treatment retards passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1[1].
    BI8622 (0-50 μM, 16 hours) retards the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells[1].
    BI8622 inhibits MYC-dependent transactivation in colorectal cancer cells[1].
    BI8622 (1 nM-10 μM) inhibits HUWE1 with an IC50 of 3.1 μM[1].
    BI8622 (5-25 μM) suppresses colony formation of Ls174T cells[1].
    BI8622 results in higher TTBK2 levels in RPE1 cells[5].

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

    BI8622 関連抗体

    Cell Cycle Analysis[1]

    Cell Line: Ls174T cells
    Concentration: 0 μM, 5 μM,10 μM, 15 μM, 20 μM
    Incubation Time: 0-4 days
    Result: Retarded passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1.

    Western Blot Analysis[1]

    Cell Line: HeLa cells
    Concentration: 0 μM, 10 μM, 20 μM
    Incubation Time: 16 hours
    Result: Retarded the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells.
    体内実験

    BI8622 (5 mg/kg, i.p., 6 h before cisplasin then once daily) significantly ameliorates cisplatin-induced renal dysfunction in cisplatin-induced AKI mouse model[4].

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

    Animal Model: Cisplatin-induced AKI mouse model<[4]
    Dosage: 5 mg/kg
    Administration: Intraperitoneal injection (i.p.), 6 h before cisplasin then once daily
    Result: Markedly decreased cisplstin-induced NGAL and KIM-1 protein levels.
    Greatly ameliorated cisplastin-induced DNA damage.
    Upregulated the protein levels of MUTYH.
    分子量

    426.51

    分子式

    C25H26N6O
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=NC=NC(N2CCC(C3=CC=CC=C3)(C#N)CC2)=C1C)NC4=CC=C(CN)C=C4
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 125 mg/mL (293.08 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 2.3446 mL 11.7231 mL 23.4461 mL
    5 mM 0.4689 mL 2.3446 mL 4.6892 mL
    10 mM 0.2345 mL 1.1723 mL 2.3446 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    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 (4.88 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 (4.88 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.
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    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.
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    純度とドキュメンテーション
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3446 mL 11.7231 mL 23.4461 mL 58.6153 mL
    5 mM 0.4689 mL 2.3446 mL 4.6892 mL 11.7231 mL
    10 mM 0.2345 mL 1.1723 mL 2.3446 mL 5.8615 mL
    15 mM 0.1563 mL 0.7815 mL 1.5631 mL 3.9077 mL
    20 mM 0.1172 mL 0.5862 mL 1.1723 mL 2.9308 mL
    25 mM 0.0938 mL 0.4689 mL 0.9378 mL 2.3446 mL
    30 mM 0.0782 mL 0.3908 mL 0.7815 mL 1.9538 mL
    40 mM 0.0586 mL 0.2931 mL 0.5862 mL 1.4654 mL
    50 mM 0.0469 mL 0.2345 mL 0.4689 mL 1.1723 mL
    60 mM 0.0391 mL 0.1954 mL 0.3908 mL 0.9769 mL
    80 mM 0.0293 mL 0.1465 mL 0.2931 mL 0.7327 mL
    100 mM 0.0234 mL 0.1172 mL 0.2345 mL 0.5862 mL
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    BI8622 Related Classifications

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    • 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:

    BI86221875036-74-0BI 8622BI-8622E1/E2/E3 Enzymec-MycE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseMycInhibitorinhibitorinhibit

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    製品名:
    BI8622
    製品番号:
    HY-120929
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