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Indisulam (E 7070) is a carbonic anhydrase inhibitor and antitumor CDK inhibitor that targets the G1 phase of the cell cycle by depleting cyclin E, inducing p53 and p21, and inhibiting CDK2, thereby causing a blockade in the G1/S transition.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $30 | In Stock | |
2 mg | $38 | In Stock | |
5 mg | $61 | In Stock | |
10 mg | $85 | In Stock | |
25 mg | $139 | In Stock | |
50 mg | $220 | In Stock | |
100 mg | $331 | In Stock | |
1 mL x 10 mM (in DMSO) | $66 | In Stock |
Description | Indisulam (E 7070) is a carbonic anhydrase inhibitor and antitumor CDK inhibitor that targets the G1 phase of the cell cycle by depleting cyclin E, inducing p53 and p21, and inhibiting CDK2, thereby 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. |
Alias | E 7070 |
Molecular Weight | 385.85 |
Formula | C14H12ClN3O4S2 |
Cas No. | 165668-41-7 |
Smiles | NS(=O)(=O)c1ccc(cc1)S(=O)(=O)Nc1cccc2c(Cl)c[nH]c12 |
Relative Density. | 1.663g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO: 20 mg/mL, clear |
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