1. PROTAC Metabolic Enzyme/Protease
  2. Molecular Glues Carbonic Anhydrase
  3. Indisulam

Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15.

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

CAS No. : 165668-41-7

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10 mM * 1 mL in DMSO
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Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Indisulam:

Top Publications Citing Use of Products

    Indisulam purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 Jul 24;43(1):205.  [Abstract]

    Fluorescence microscopy images of the T-ALL cell lines J.gamma1 and Jurkat after 48 h of treatment with 1 μM and 5 μM Indisulam, respectively.

    Indisulam purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 Jul 24;43(1):205.  [Abstract]

    Flow cytometry analysis was performed to assess apoptosis in T-ALL cells after 24 h of treatment with DMSO or various concentrations of Indisulam (1 μM and 5 μM) utilizing Annexin V and PI staining. The percentage of apoptotic cells was subjected to statistical evaluation.

    Indisulam purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 Jul 24;43(1):205.  [Abstract]

    Western blot analysis was performed to validate the protein expression changes occurring in the J.gamma1 and Jurkat cell lines after treatment with Indisulam (1 μM and 5 μM) for 24 and 48 h, respectively.

    Indisulam purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 Jul 24;43(1):205.  [Abstract]

    Compared with the control group, the Indisulam (12.5 mg/kg, i.p.)-treated group displayed a significant decrease in fluorescence intensity at four distinct time points posttreatment, demonstrating a substantial suppression of J.gamma1 cell proliferation in vivo.

    Indisulam purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2024 Jul 24;43(1):205.  [Abstract]

    Immunohistochemical analyses of the Indisulam (12.5 mg/kg, i.p.)-treated group the mouse bone, liver, and spleen tissues revealed a decreased expression of Ki67 and RBM39.

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    • Purity & Documentation

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    • Customer Review

    Description

    Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15[1][2].

    IC50 & Target

    Carbonic anhydrase[1].

    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    0.21 μM
    Compound: 3
    Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in HCT116-C9 cell line
    Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in HCT116-C9 cell line
    [PMID: 12383017]
    HCT-116 IC50
    29 μM
    Compound: 3
    Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in HCT116-C9 -C1cell line
    Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in HCT116-C9 -C1cell line
    [PMID: 12383017]
    KB IC50
    4.4 μg/mL
    Compound: 25(E7070)
    Antiproliferative activity against KB human nasopharynx carcinoma in vitro
    Antiproliferative activity against KB human nasopharynx carcinoma in vitro
    [PMID: 10508428]
    MC-38 IC50
    0.1 μg/mL
    Compound: 25(E7070)
    In vitro antiproliferative activity against colon 38 murine adenocarcinoma
    In vitro antiproliferative activity against colon 38 murine adenocarcinoma
    [PMID: 10508428]
    MCF7 IC50
    36.3 μM
    Compound: E7070
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation incubated for 48 hrs by Sulfo-Rhodamine-B stain (SRB) assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation incubated for 48 hrs by Sulfo-Rhodamine-B stain (SRB) assay
    [PMID: 32707525]
    P388 IC50
    0.45 μg/mL
    Compound: 25(E7070)
    Antiproliferative activity against P388 murine leukemia in vitro
    Antiproliferative activity against P388 murine leukemia in vitro
    [PMID: 10508428]
    P388 IC50
    0.59 μM
    Compound: 3
    Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388/4.0 r-M cell line
    Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388/4.0 r-M cell line
    [PMID: 12383017]
    P388 IC50
    0.61 μM
    Compound: 3
    Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388 cell line
    Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388 cell line
    [PMID: 12383017]
    In Vitro

    Indisulam (E7070, 0-50 μg/mL, 12-48 h) causes cell cycle perturbation in the G1 phase in a time- and dose-dependent manner, potentially leading to cell death[1].

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

    Cell Cycle Analysis[1]

    Cell Line: P388 murine leukaemia cells.
    Concentration: 0-50 μg/mL.
    Incubation Time: 12-48 h.
    Result: Accumulated P388 cells in the G1 phase.
    In Vivo

    Indisulam (E7070, 12.5, 25, 50 (100) mg/kg) shows an antitumour spectrum in human cancer models[1].

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

    Animal Model: Female BALB/c nu/nu mice aged 7 weeks (HCT116 colon, LX-1 lung, SW620 colon, HCT115 colon, PC-9 lung, DLD-1 colon and WiDr colon models)[1].
    Dosage: 12.5, 25, 50 (100) mg/kg.
    Administration: IV daily for 4 days.
    Result: Exhibited anti-tumor activity.
    Clinical Trial
    Molecular Weight

    385.85

    Formula

    C14H12ClN3O4S2

    CAS No.
    Appearance

    Solid

    Color

    White to pink

    SMILES

    O=S(C1=CC=C(S(=O)(N)=O)C=C1)(NC2=CC=CC3=C2NC=C3Cl)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (259.17 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 2.5917 mL 12.9584 mL 25.9168 mL
    5 mM 0.5183 mL 2.5917 mL 5.1834 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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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: ≥ 2.17 mg/mL (5.62 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (5.62 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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)

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    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: 99.80%

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5917 mL 12.9584 mL 25.9168 mL 64.7920 mL
    5 mM 0.5183 mL 2.5917 mL 5.1834 mL 12.9584 mL
    10 mM 0.2592 mL 1.2958 mL 2.5917 mL 6.4792 mL
    15 mM 0.1728 mL 0.8639 mL 1.7278 mL 4.3195 mL
    20 mM 0.1296 mL 0.6479 mL 1.2958 mL 3.2396 mL
    25 mM 0.1037 mL 0.5183 mL 1.0367 mL 2.5917 mL
    30 mM 0.0864 mL 0.4319 mL 0.8639 mL 2.1597 mL
    40 mM 0.0648 mL 0.3240 mL 0.6479 mL 1.6198 mL
    50 mM 0.0518 mL 0.2592 mL 0.5183 mL 1.2958 mL
    60 mM 0.0432 mL 0.2160 mL 0.4319 mL 1.0799 mL
    80 mM 0.0324 mL 0.1620 mL 0.3240 mL 0.8099 mL
    100 mM 0.0259 mL 0.1296 mL 0.2592 mL 0.6479 mL
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      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.

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    Product Name:
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    Cat. No.:
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