2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK
  3. E1/E2/E3 Enzyme TAM Receptor
  4. 2-D08

2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC50 of 0.49 nM.

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

2-D08 Chemical Structure

2-D08 Chemical Structure

CAS No. : 144707-18-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 73 In-stock
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5 mg USD 66 In-stock
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25 mg USD 231 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

2-D08 Related Antibodies

Top Publications Citing Use of Products

    2-D08 purchased from MedChemExpress. Usage Cited in: Life Sci. 2020 Aug 15;255:117859.  [Abstract]

    The expression levels of TGF-β/SMAD and HIF-1 signaling pathways-related proteins, including Col III, Smad2, Smad3, Smad4 and HIF-1α are measured by western blotting in HFFs and HKFs. The band intensity ratio of the TGF-β/SMAD and HIF-1 signaling related protein to reference protein is significantly decreased in the 2-D08 group.

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    Axl Mer Tyro3

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC50 of 0.49 nM.

    IC50 & Target

    Axl

     

    In Vitro

    2-D08 inhibits sumoylation by preventing transfer of SUMO from the UBC9-SUMO thioester to the substrate[1]. 2-D08 decreases the ratio of p-Axl to t-Axl in a dose-dependent manner. Suppression of Axl kinase activity by 2D08 disrupts the cytoskeleton and actin filaments with re-organization at cellular junctions[2].

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

    2-D08 Related Antibodies
    Molecular Weight

    270.24

    Formula

    C15H10O5
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C=C(C2=CC=C(O)C(O)=C2O)OC3=CC=CC=C13
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 150 mg/mL (555.06 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 3.7004 mL 18.5021 mL 37.0041 mL
    5 mM 0.7401 mL 3.7004 mL 7.4008 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 (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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)

    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 (9.25 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 (9.25 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 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).

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    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: 99.17%

    SDS (392 KB)

    COA (250 KB) HNMR (259 KB) RP-HPLC (246 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Human lung multi-potent cells at passage 5 are incubated with DMEM+0.5% BSA+penicillin/streptomycin containing either 0.1% DMSO (vehicle) or 2D08 (10 μM) on Permanox culture slides for 6 days. Cells are fixed with 4% PFA for 30 min and then blocked and permeabilized with 10% goat serum and 0.3% Triton-X 100 in PBS for 30 min[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice[3]

    Eight- to 10-week-old mice (both male and female) are used for the study. A 5 cm-long glass pipette is buffered with Mineral Oil and then attached to the injection apparatus to take up 10 μL of 2-D08 (30 μM) or NaCl[3].

    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, 2 years; -20°C, 1 year (protect from light). 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 3.7004 mL 18.5021 mL 37.0041 mL 92.5104 mL
    5 mM 0.7401 mL 3.7004 mL 7.4008 mL 18.5021 mL
    10 mM 0.3700 mL 1.8502 mL 3.7004 mL 9.2510 mL
    15 mM 0.2467 mL 1.2335 mL 2.4669 mL 6.1674 mL
    20 mM 0.1850 mL 0.9251 mL 1.8502 mL 4.6255 mL
    25 mM 0.1480 mL 0.7401 mL 1.4802 mL 3.7004 mL
    30 mM 0.1233 mL 0.6167 mL 1.2335 mL 3.0837 mL
    40 mM 0.0925 mL 0.4626 mL 0.9251 mL 2.3128 mL
    50 mM 0.0740 mL 0.3700 mL 0.7401 mL 1.8502 mL
    60 mM 0.0617 mL 0.3084 mL 0.6167 mL 1.5418 mL
    80 mM 0.0463 mL 0.2313 mL 0.4626 mL 1.1564 mL
    100 mM 0.0370 mL 0.1850 mL 0.3700 mL 0.9251 mL
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    2-D08 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:

    2-D08144707-18-6E1/E2/E3 EnzymeTAM ReceptorE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseTyro3AxlMerInhibitorinhibitorinhibit

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    Product Name:
    2-D08
    Cat. No.:
    HY-114166
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