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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- CAS No.: 3113303-04-8
- 화학식: C21H22N6O2
- 분자량:390.44
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
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PRMT5 ≥ 9.7 (pIC50) |
PRMT5-IN-53 (Compound 9) inhibits global SDMA methylation in A549 cells with an pIC50 value of 9.4 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Vdss | T1/2 | Brain-to-Plasma Ratio | CL | F |
|---|---|---|---|---|---|---|---|
| Dog[1] | 0.5 mg/kg | i.v. | 11 L/kg | 9.3 h | 1.7 | / | / |
| Dog[1] | 5 mg/kg | p.o. | / | / | / | 30 mL/min/kg | 0.6 % |
| Mice[1] | 0.5 mg/kg | i.v. | 3.2 L/kg | 0.41 h | 1.3 | / | / |
| Mice[1] | 50 mg/kg | p.o. | / | / | / | 196 mL/min/kg | 0.05 % |
| Rat[1] | 0.5 mg/kg | i.v. | 4.6 L/kg | 2.3 h | 1.6 | / | / |
| Rat[1] | 100 mg/kg | p.o. | / | / | / | 65 mL/min/kg | 0.03 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DSS-induced polyp-bearing model established in Female ApcMin/+ (C57BL/6J-ApcMin/J, aged 4−5 weeks)[1]
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Dosage:25 and 75 mg/kg
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Administration:Intragastric administration (i.g.), twice daily for 14-21 days
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Result:Significantly reduced SDMA and SmD3-Me2 during 2 weeks in the colon tissue, bone marrow and spleen showed no changes in SDMA signals during 1 week.
Reduced the number and size of polyps during 3 weeks.
Did not cause systemic targeted toxicity.
Chemical Information
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CAS No. 3113303-04-8
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분자량 390.44
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화학식 C21H22N6O2
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PRMT5-IN-53 Related Classifications
HY-178028 Related Classifications
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