Indisulam (Synonyms: E-7070) |
Catalog No.GC65549
One-Click Copy Product Info
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Indisulam is a sulfonamide anticancer agent and molecular glue degrader. Indisulam binds to the CUL4-DCAF15 E3 ubiquitin ligase complex, thereby inducing proteasomal degradation of the RNA-binding motif protein 39 (RBM39). Indisulam also inhibits carbonic anhydrase and arrests the cell cycle in the G1 phase.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 165668-41-7
Sample solution is provided at 25 µL, 10mM.
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Indisulam is a sulfonamide anticancer agent and molecular glue degrader. Indisulam binds to the CUL4-DCAF15 E3 ubiquitin ligase complex, thereby inducing proteasomal degradation of the RNA-binding motif protein 39 (RBM39). Indisulam also inhibits carbonic anhydrase and arrests the cell cycle in the G1 phase[1-2]. Indisulam is used in research related to solid tumors, acute myeloid leukemia, and multiple myeloma[3-4].
In vitro, cells were pretreated with Indisulam (0.5-2μM) for 30 minutes to 2 hours, followed by LLS stimulation for 5.5 hours. Indisulam induced the degradation of the RNA-binding protein RBM39 and downregulated cyclin H, thereby inhibiting CDK2 activation[5]. Human cervical cancer cell lines (HeLa and C33A) were treated with Indisulam (0-10μM) for 24-72 hours. Indisulam induced RBM39 degradation and caused aberrant RNA splicing, specifically altering the ratio of apoptotic regulator p73 splice isoforms (ΔNp73 and TAp73). Indisulam significantly inhibited cell growth and proliferation and induced apoptosis[6].
In vivo, a cholangiocarcinoma mouse model was treated with Indisulam (15mg/kg; intraperitoneal injection) three times a week for a total of seven doses. Indisulam significantly reduced tumor burden (as evidenced by a decreased liver weight/body weight ratio) and tumor cell proliferation[7]. In an acute megakaryoblastic leukemia (AMKL) mouse model established by tail vein injection of luciferase-expressing CMK cells, the mice were treated with Indisulam (25mg/kg/day) for 7 days. Indisulam significantly reduced the leukemic burden in the spleen, liver, and bones (femur and tibia), and decreased the proportions of Ki67-positive cells and CD45+ leukemia cells in the bone marrow, spleen, and liver tissues[8].
References:
[1] Ozawa Y, Sugi NH, Nagasu T, 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.
[2] Abbate F, Casini A, Owa T, 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.
[3] Lu SX, De Neef E, Thomas JD, et al. Pharmacologic modulation of RNA splicing enhances anti-tumor immunity. Cell. 2021 Jul 22;184(15):4032-4047.e31.
[4] Han T, Goralski M, Gaskill N, et al. Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15. Science. 2017 Apr 28;356(6336):eaal3755.
[5] Pogacar Z, Johnson JL, Krenning L, et al. Indisulam synergizes with palbociclib to induce senescence through inhibition of CDK2 kinase activity. PLoS One. 2022 Sep 6;17(9):e0273182.
[6] Dou Z, Zhang X, Su W, et al. Indisulam exerts anticancer effects via modulation of transcription, translation and alternative splicing on human cervical cancer cells. Am J Cancer Res. 2023 Jul 15;13(7):2922-2937.
[7] Liu N, Zhang J, Chen W, et al. RBM39 Enhances Cholangiocarcinoma Growth Through EZH2-mediated WNT7B/β-catenin Pathway. Cell Mol Gastroenterol Hepatol. 2025;19(1):101404.
[8] Yang Y, Li Z, Yang Y, et al. The RBM39 degrader indisulam inhibits acute megakaryoblastic leukemia by altering the alternative splicing of ZMYND8. Cell Biosci. 2025 Apr 13;15(1):46. doi: 10.1186/s13578-025-01380-3.
| Cell experiment [1]: | |
Cell lines | HeLa cells (human cervical adenocarcinoma cell line) and C33A cells (human cervical squamous cell carcinoma cell line) |
Preparation Method | Both HeLa and C33A cells were cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO2. The cells were treated with increasing concentrations of Indisulam for 24, 48, and 72 hours. |
Reaction Conditions | 0-10μM; 24h-72h. |
Applications | Indisulam treatment significantly inhibited the growth and viability of HeLa and C33A cells in a time- and dose-dependent manner. Indisulam induced proteasomal degradation of the splicing factor RBM39, leading to widespread transcriptional and translational perturbations. Indisulam disrupted RNA splicing, causing aberrant alternative splicing events, including altered splicing of p73 isoforms, increasing the pro-apoptotic TAp73 and decreasing the anti-apoptotic ΔNp73. This triggered the intrinsic mitochondrial apoptosis pathway, characterized by an increased Bax/Bcl-2 ratio, cytochrome c release, and activation of caspase-3. |
| Animal experiment [2]: | |
Animal models | NOD/SCID/IL2Rγ⁻¹/¹ (NSG) female mice |
Preparation Method | The mice were intravenously injected with CMK leukemia cells expressing firefly luciferase (1×10⁶ cells per mouse). Ten days after cell injection, mice were treated with Indisulam (25mg/kg/day). |
Dosage form | 25mg/kg/day; i.p.; 7 day. |
Applications | Indisulam treatment in DCAF15 wild-type mice significantly reduced the leukemic burden (as measured by bioluminescence intensity) in the spleen, liver, and bones. It decreased the number of proliferating (Ki67-positive) leukemia cells and human CD45+ leukemia cells infiltrating the bone marrow, spleen, and liver. Indisulam treatment significantly prolonged the overall survival of the leukemic mice compared to the vehicle control group. Importantly, no significant drug toxicity was observed during the treatment period. The efficacy of Indisulam was dependent on DCAF15 expression, as its anti-leukemic effects were abrogated in DCAF15 knockout mice. |
References: | |
| Cas No. | 165668-41-7 | SDF | |
| Synonyms | E-7070 | ||
| Formula | C14H12ClN3O4S2 | M.Wt | 385.85 |
| Solubility | DMSO : 100 mg/mL (259.17 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5917 mL | 12.9584 mL | 25.9168 mL |
| 5 mM | 518.3 μL | 2.5917 mL | 5.1834 mL |
| 10 mM | 259.2 μL | 1.2958 mL | 2.5917 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)