PRMT5-IN-53

PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD 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) [1].

Product Specifications

UNSPSC

12352005

Target

Histone Methyltransferase

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O[C@@H]1[C@H](O)[C@@H](CNC2=CC=C(C=CC(N)=N3)C3=C2)C[C@H]1N(C=C4)C5=C4C=NC=N5

Molecular Formula

C21H22N6O2

Molecular Weight

390.44

References & Citations

[1]Hulpia F, et al. Discovery of Gut-Restricted PRMT5 Inhibitors to Intercept Colorectal Cancer in Patients with Genetic Loss of Tumor Suppressor Adenomatous Polyposis Coli. J Med Chem. 2025 Aug 26.