PRMT5-IN-53

• Description:

  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].

• 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.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  PRMT5