3113303-04-8
Chemical Structure
PRMT5-IN-53
- CAS No.: 3113303-04-8
- Formula:C21H22N6O2
- Molecular Weight:390.44
IUPAC Name: (1S,2R,3R,5R)-3-(((2-aminoquinolin-7-yl)amino)methyl)-5-(7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol
InChIKey: YGLBDQDJLKNOTG-JRJVTICQSA-N
SMILES: O[C@H]1[C@@H](C[C@@H]([C@H]1O)CNC2=CC3=C(C=CC(N)=N3)C=C2)N4C5=NC=NC=C5C=C4
Biological Activity: 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].
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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). | |||||||||||||||||||||
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Keywords
