Indisulam
Based on 15 publication(s) in Google Scholar
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.
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- 純度: 99.80%
- CAS 番号: 165668-41-7
- 分子式: C14H12ClN3O4S2
- 分子量:385.85
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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MedChemExpress（MCE）の使用を引用している文献 Indisulam
More- Nat Chem Biol. 2023 Dec;19(12):1513-1523. [Abstract]
- J Exp Clin Cancer Res. 2024 Jul 24;43(1):205. [Abstract]
- J Exp Clin Cancer Res. 2023 Aug 21;42(1):214. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2024 Sep 13:101404. [Abstract]
- Oncogene. 2025 Jun;44(20):1488-1503. [Abstract]
- Cell Rep. 2024 Sep 13;43(9):114751. [Abstract]
- Cell Biosci. 2025 Apr 13;15(1):46. [Abstract]
- Cell Prolif. 2025 May 13:e70059. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2024 Jan;1871(1):119607. [Abstract]
- Bioorg Med Chem. 2020 Oct 15;28(20):115712. [Abstract]
- PLoS One. 2024 Apr 9;19(4):e0299019. [Abstract]
- bioRxiv. 2025 Sep 2:2022.10.31.514544. [Abstract]
- bioRxiv. 2024 Jul 25.
- SSRN. 2024 Jun 19.
- University of Munich. 2022 Oct.
Customer Validation & Images
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Cell Imaging/Staining
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Apoptosis Analysis
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WB
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In Vivo Efficacy Study
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IHC
生物活性
Carbonic anhydrase[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.21 μM
Compound: 3
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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
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[PMID: 12383017] |
| HCT-116 | IC50 |
29 μM
Compound: 3
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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
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[PMID: 12383017] |
| KB | IC50 |
4.4 μg/mL
Compound: 25(E7070)
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Antiproliferative activity against KB human nasopharynx carcinoma in vitro
Antiproliferative activity against KB human nasopharynx carcinoma in vitro
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[PMID: 10508428] |
| MC-38 | IC50 |
0.1 μg/mL
Compound: 25(E7070)
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In vitro antiproliferative activity against colon 38 murine adenocarcinoma
In vitro antiproliferative activity against colon 38 murine adenocarcinoma
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[PMID: 10508428] |
| MCF7 | IC50 |
36.3 μM
Compound: E7070
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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
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[PMID: 32707525] |
| P388 | IC50 |
0.45 μg/mL
Compound: 25(E7070)
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Antiproliferative activity against P388 murine leukemia in vitro
Antiproliferative activity against P388 murine leukemia in vitro
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[PMID: 10508428] |
| P388 | IC50 |
0.59 μM
Compound: 3
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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
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[PMID: 12383017] |
| P388 | IC50 |
0.61 μM
Compound: 3
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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
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[PMID: 12383017] |
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.
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Cell Line:P388 murine leukaemia cells.
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Concentration:0-50 μg/mL.
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Incubation Time:12-48 h.
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Result:Accumulated P388 cells in the G1 phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
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Dosage:12.5, 25, 50 (100) mg/kg.
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Administration:IV daily for 4 days.
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Result:Exhibited anti-tumor activity.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 165668-41-7
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性状 Solid
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分子量 385.85
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分子式 C14H12ClN3O4S2
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Color White to pink
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SMILES
O=S(C1=CC=C(S(=O)(N)=O)C=C1)(NC2=CC=CC3=C2NC=C3Cl)=O
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別名
インジスラム; E 7070
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 1 year -20°C 6 months
Publications (15)
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Journal Impact Factor
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Most Recent
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Nat Chem Biol
2023 Dec;19(12):1513-1523. PMID: 37653169 -
J Exp Clin Cancer Res
Targeting RBM39 through indisulam induced mis-splicing of mRNA to exert anti-cancer effects in T-cell acute lymphoblastic leukemia. [Abstract]2024 Jul 24;43(1):205. PMID: 39044280
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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J Exp Clin Cancer Res
MYC up-regulation confers vulnerability to dual inhibition of CDK12 and CDK13 in high-risk Group 3 medulloblastoma. [Abstract]2023 Aug 21;42(1):214. PMID: 37599362 -
Cell Mol Gastroenterol Hepatol
2024 Sep 13:101404. PMID: 39278404 -
Oncogene
RBM39 promotes hepatocarcinogenesis by regulating RFX1's alternative splicing and subsequent activation of integrin signaling pathway. [Abstract]2025 Jun;44(20):1488-1503. PMID: 40033026 -
Cell Rep
Transient splicing inhibition causes persistent DNA damage and chemotherapy vulnerability in triple-negative breast cancer. [Abstract]2024 Sep 13;43(9):114751. PMID: 39276346 -
Cell Biosci
The RBM39 degrader indisulam inhibits acute megakaryoblastic leukemia by altering the alternative splicing of ZMYND8. [Abstract]2025 Apr 13;15(1):46. PMID: 40223119 -
Cell Prolif
RBM39 Promotes Base Excision Repair to Facilitate the Progression of HCC by Stabilising OGG1 mRNA. [Abstract]2025 May 13:e70059. PMID: 40364450 -
Biochim Biophys Acta Mol Cell Res
Regulatory role of RBM39 in acute myeloid leukemia: Mediation through the PI3K/AKT pathway. [Abstract]2024 Jan;1871(1):119607. PMID: 37852323 -
Bioorg Med Chem
2020 Oct 15;28(20):115712. PMID: 33069070 -
PLoS One
Indisulam synergizes with melphalan to inhibit Multiple Myeloma malignancy via targeting TOP2A. [Abstract]2024 Apr 9;19(4):e0299019. PMID: 38593113 -
bioRxiv
2025 Sep 2:2022.10.31.514544. PMID: 40950106 -
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溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
Please enter the basic information of animal experiments:
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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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
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参考文献
[1]. Ozawa Y, et al. E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo. Eur J Cancer. 2001 Nov;37(17):2275-82. [Content Brief]
[2]. Abbate F, et al. Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Bioorg Med Chem Lett. 2004 Jan 5;14(1):217-23. [Content Brief]
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 |
Indisulam 関連分類
HY-13650 関連分類
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