TASIN-1

TASIN-1 is a small molecule that selectively inhibits mutant (truncated) adenomatous polyposis coli (APC), a tumor suppressor gene frequently mutated in colorectal cancer. It exerts its cytotoxic effects by inhibiting emopamil-binding protein (EBP), an enzyme involved in cholesterol biosynthesis. This inhibition leads to depletion of cellular cholesterol levels and induces apoptotic cell death specifically in colorectal cancer cells harboring truncated APC mutations. The mechanism involves activation of endoplasmic reticulum (ER) stress-dependent JNK signaling and production of reactive oxygen species (ROS), as well as inhibition of AKT pro-survival signaling. In preclinical models—including human colon tumor xenografts and genetically engineered mouse models—TASIN-1 significantly reduced tumor growth with minimal toxicity to normal tissues[2][3][4][5][6].

Other names

Truncated APC Selective INhibitor-11'-[(4-Methoxyphenyl)sulfonyl]-4-methyl-1,4'-bipiperidine hydrochloride