Indisulam 是碳酸酐酶抑制剂。它是细胞周期G1期的靶向化合物，能够抑制CDK2及周期蛋白 E的激活，阻止 G1/S 的转化。它可以募集DCAF15诱导RBM39降解来靶向剪接，具有抗癌作用。

Indisulam 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, 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.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.

165668-41-7

C14H12ClN3O4S2

385.84

E 7070

DMSO:20 mg/mL, clear
Powder: -20°C for 3 years
In solvent: -80°C for 2 years