Indisulam

Indisulam is a sulfonamide with anticancer activity.¹ 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, 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.² It is also an inhibitor of carbonic anhydrase in H. pylori (K_i = 310-562 nM).³

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1. Ozawa, Y., Sugi, N.H., Nagasu, T., et al. E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo. Eur. J. Cancer 37(17), 2275-2282 (2001).

2. Han, T., Goralski, M., Gaskill, N., et al. Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15. Science 356(6336), (2017).

3. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).