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
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
PRMT5
Frequently Asked Questions
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