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Indisulam

Catalog No. T4321 CAS 165668-41-7

Synonyms: E 7070

Indisulam (E 7070) is a carbonic anhydrase inibitor and Antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition.

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Indisulam, CAS 165668-41-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 38.00
5 mg	In stock	$ 61.00
10 mg	In stock	$ 85.00
25 mg	In stock	$ 139.00
50 mg	In stock	$ 220.00
100 mg	In stock	$ 331.00
1 mL * 10 mM (in DMSO)	In stock	$ 66.00

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Purity: 99.77%

Purity: 99.21%

Purity: 99.07%

Purity: 98.93%

Purity: 98.68%

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Storage & Solubility Information

Description	Indisulam (E 7070) is a carbonic anhydrase inibitor and Antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition.
In vitro	In vitro, indisulam has antiproliferative effects on a wide range of human tumor lines with HCT116 colorectal being the most sensitive and NCI-H596 non-small cell lung cancer (NSCLC) the most resistant (IC50s = 0.11 and 94 μg/ml, respectively). It increases the number of P388 murine leukemia cells in the G1 phase of the cell cycle in a dose-dependent manner and exerts time-dependent cytotoxicity against HCT116 cells.
In vivo	In vivo, indisulam suppresses tumor growth and decreases tumor volume in murine HCT116, SW620, and HCT15 colorectal and LX-1 and PC9 lung cancer xenograft models. Indisulam induces proteasomal degradation of RNA binding motif protein 39 (RBM39) through association with the CUL4-DCAF15 E3 ubiquitin ligase in vitro.It is also an inhibitor of carbonic anhydrase in H. pylori (Ki = 310-562 nM). Formulations containing indisulam are under Clinicalal investigation for the treatment of solid tumors.

Synonyms	E 7070
Molecular Weight	385.85
Formula	C14H12ClN3O4S2
CAS No.	165668-41-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 20 mg/mL, clear

References and Literature

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. 2. Han T,etal.Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15. Science. 2017 Apr 28;356(6336). 3. Nishimori I,et al.Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori.Bioorg Med Chem Lett. 2006 Apr 15;16(8):2182-8. 4. Siegel-Lakhai WS,etal.A dose-escalation study of indisulam in combination with capecitabine (Xeloda) in patients with solid tumours.Br J Cancer. 2008 Apr 22;98(8):1320-6.

Citations

1. Lu J, Jiang H, Li D, et al. Proximity Labeling, Quantitative Proteomics, and Biochemical Studies Revealed the Molecular Mechanism for the Inhibitory Effect of Indisulam on the Proliferation of Gastric Cancer Cells. Journal of Proteome Research. 2021 2. Lu J, Li D, Jiang H, et al.The aryl sulfonamide indisulam inhibits gastric cancer cell migration by promoting the ubiquitination and degradation of the transcription factor ZEB1.Journal of Biological Chemistry.2023: 103025. 3. Hou C, Wu X, Shi R, et al.Subtle structural alteration in indisulam switches the molecular mechanisms for the inhibitory effect on the migration of gastric cancer cells.Biomedicine & Pharmacotherapy.2024, 172: 116259.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library NO PAINS Compound Library Anti-Pancreatic Cancer Compound Library ReFRAME Related Library Anti-Colorectal Cancer Compound Library Anti-Metabolism Disease Compound Library

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Keywords

Indisulam 165668-41-7 Cell Cycle/Checkpoint Metabolism Carbonic Anhydrase CDK E7070 E-7070 Inhibitor E 7070 Carbonate dehydratase inhibit inhibitor

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