U-CH3

U-CH3 is a small molecule ureido-substituted benzene sulfonamide (USB) that acts as a potent and selective inhibitor of the tumor-associated carbonic anhydrase isoforms IX (CA IX) and XII (CA XII). It functions by binding to the catalytic zinc ion within the enzyme's active site via its sulfonamide moiety and interacting with a "selective pocket" (specifically residue 131), which provides significant selectivity over the off-target cytosolic isoform CA II. In preclinical breast cancer models, U-CH3 has demonstrated the ability to inhibit cell growth, migration, and invasion, particularly in triple-negative breast cancer (TNBC) and ER-positive cell lines. Research indicates a notable disconnect between its high affinity for purified recombinant proteins and the significantly higher concentrations required to achieve growth inhibition in intact cells, suggesting that its anti-proliferative effects may involve mechanisms beyond simple exofacial CA inhibition.

Other names

ureido-substituted benzene sulfonamide