polyposis

Demethyl celecoxib is a selective inhibitor of COX-2 with anti-inflammatory activity (IC50 of 32 nM). with anti-inflammatory activities. Desmethyl Celecoxib is an analog of Celecoxib and with the optimal yield of 75%.

PRMT5-IN-53 is an orally active, gut-restricted PRMT5 inhibitor, exhibiting pIC50 values of ≥ 9.7 against both hPRMT5 and mPRMT5. It binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. In mice, PRMT5-IN-53 effectively inhibits intestinal PRMT5, significantly reducing both the number and size of polyps while avoiding systemic hematologic toxicity such as anemia and neutropenia. This compound is applicable in colorectal cancer research, particularly for familial adenomatous polyposis (FAP).

TASIN-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (APC).

MAIT-203, a cyclopentyalanin-derived peptidomimetic, effectively disrupts the interaction between adenomatous polyposis coli (APC) and Asef (RhoGEF4), without affecting APC-Sam68 or APC-striatin interactions. It binds to APC-ARM domains with a K i of 0.015 μM and a K d of 0.036 μM, notably inhibiting the migration and invasion of colorectal cancer cells.

MAIT-203 acetate is a cyclopentylglycine-derived peptidomimetic that effectively inhibits the interaction between adenomatous polyposis coli (APC) and Asef (RhoGEF4), while not affecting the APC-Sam68 or APC-striatin interactions. It binds to APC-ARM with a Ki of 0.015 μM and a Kd of 0.036 μM, significantly impeding the migration and invasion of colorectal cancer cells.