After screening series of arylsulfonamide derivatives, we found that MPT0B390 (3-[1-(3,4-dimethoxy-benzenesulfonyl)-1H-indol-5-yl]-N-hydroxy-acrylamide) can significantly upregulate TIMP3 expression in colorectal cancer cells and exhibit potent anti-tumor, anti-metastasis and anti-angiogenic effect in vivo, which indicates the potential usage of MPT0B390 as a therapeutic agent with multiple inhibitory aspects against colorectal cancer growth and angiogenesis. The gene discussed is TIMP3; the disease is colorectal cancer.