PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC 50 s of ≥ 9.7 against hPRMT5 and mPRMT5 . PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a K D of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis ( FAP ).
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