2. Cell Cycle/DNA Damage
  3. APC
  4. Apcin

Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis.

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Apcin Chemical Structure

Apcin Chemical Structure

CAS No. : 300815-04-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
1 mg USD 52 In-stock
5 mg USD 110 In-stock
10 mg USD 176 In-stock
25 mg USD 352 In-stock
50 mg USD 616 In-stock
100 mg USD 1078 In-stock
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Based on 6 publication(s) in Google Scholar

Apcin Related Antibodies

Top Publications Citing Use of Products

    Apcin purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2023 Feb 9;1869(4):166663.  [Abstract]

    Apcin (5 mg/kg; i.p.; single daily for 7 days) significantly attenuates both Collagen I and Collagen III in a renal fibrosis animal model (unilateral ureteral obstruction, UUO), and decreases the level of profibrotic factor TGF-β1.

    • Biological Activity

    • Purity & Documentation

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    Description

    Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis[1][2][3].

    In Vitro

    Apcin (25-50 μM; 48 hours) significantly increases MM apoptosis combining with proTAME (6, 12 μM)[3].
    ? Apcin (25 μM; 2-14 hours) induces slippage more slowly[2].
    ? Apcin (50-200 μM) stabilizes cycB1-NT and securin most effectively, with somewhat weaker effects against full-length cyclin B1[1].
    ? Apcin (1.5-200 μM; 18 hours) synergizes with proTAME (a cell-permeable TAME prodrug) to prolong mitotic duration in RPE1 cells[1].

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

    Apcin Related Antibodies

    Apoptosis Analysis[3]

    Cell Line: HMCLs LP-1 and RPMI-8226 cells
    Concentration: 25, 50 μM
    Incubation Time: 48 hours
    Result: Had minor effects on multiple myeloma (MM) cells alone and significantly increased MM apoptosis combining with proTAME (6, 12 μM).

    Western Blot Analysis[2]

    Cell Line: HeLa cells with Nocodazole (100 nM)
    Concentration: 25 μM
    Incubation Time: 2-14 hours
    Result: Induced slippage more slowly, as indicated by Cdc27 dephosphorylation and a reduction in cyclin B1, securin and phosphoH3 levels beginning 4-6h after mitotic entry.
    Molecular Weight

    438.65

    Formula

    C13H14Cl3N7O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(OCCN1C([N+]([O-])=O)=CN=C1C)NC(NC2=NC=CC=N2)C(Cl)(Cl)Cl
    Shipping

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

    DMSO : 125 mg/mL (284.97 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 2.2797 mL 11.3986 mL 22.7972 mL
    5 mM 0.4559 mL 2.2797 mL 4.5594 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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    • 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

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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 (4.74 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 (4.74 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
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    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
    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. 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 2.2797 mL 11.3986 mL 22.7972 mL 56.9930 mL
    5 mM 0.4559 mL 2.2797 mL 4.5594 mL 11.3986 mL
    10 mM 0.2280 mL 1.1399 mL 2.2797 mL 5.6993 mL
    15 mM 0.1520 mL 0.7599 mL 1.5198 mL 3.7995 mL
    20 mM 0.1140 mL 0.5699 mL 1.1399 mL 2.8497 mL
    25 mM 0.0912 mL 0.4559 mL 0.9119 mL 2.2797 mL
    30 mM 0.0760 mL 0.3800 mL 0.7599 mL 1.8998 mL
    40 mM 0.0570 mL 0.2850 mL 0.5699 mL 1.4248 mL
    50 mM 0.0456 mL 0.2280 mL 0.4559 mL 1.1399 mL
    60 mM 0.0380 mL 0.1900 mL 0.3800 mL 0.9499 mL
    80 mM 0.0285 mL 0.1425 mL 0.2850 mL 0.7124 mL
    100 mM 0.0228 mL 0.1140 mL 0.2280 mL 0.5699 mL
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    Apcin 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:

    Apcin300815-04-7APCAnaphase promoting complexanaphase-promotingcomplexcyclosomeAPC/CCdc20E3ligaseubiquitylationrecognitionD-box-bindingpocketWD40-domainmitosisInhibitorinhibitorinhibit

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