PRMT5-MTA-IN-8
PRMT5-MTA-IN-8 is an orally active PRMT5-MTA complex inhibitor (IC50 = 4.4 nM). PRMT5-MTA-IN-8 inhibits the intracellular production of symmetric dimethylarginine (SDMA) as well as the proliferation of MTAP-deficient cells. PRMT5-MTA-IN-8 exerts antitumor efficacy by inhibiting PRMT5, reducing SDMA levels and inducing tumor cell apoptosis in mouse models of triple-negative breast cancer. PRMT5-MTA-IN-8 can be used in research related to cancers such as triple-negative breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3105952-57-3
- Formula: C19H17BrN6O2
- Molecular Weight:441.28
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
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PRMT5-MTA 4.4 nM (IC50) |
PRMT5-MTA-IN-8 (Compound I-14) inhibits PRMT5-dependent SDMA formation in HCT116 MTAP-null cells (IC50 = 0.8 nM) and suppresses the proliferation of HCT116 MTAP-null cells (IC50 = 3.9 nM)[1].
PRMT5-MTA-IN-8 (0.1-1000 nM, 6 days) inhibits PRMT5-dependent SDMA production in MDA-MB-231 cells with an IC50 of 0.25 nM, and increases the thermal stability of PRMT5[1].
PRMT5-MTA-IN-8 exhibits high metabolic stability in rat liver microsomes and plasma, with half-lives of 131 and 136 min, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0.01, 0.1, 1.0, 10, 100, and 1000 nM
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Incubation Time:6 days
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Result:Decreased global SDMA.
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Cell Line:MDA-MB-231 cells
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Concentration:0.01, 0.1, 1.0, 10, 100, and 1000 nM
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Incubation Time:6 days
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Result:Improved the thermal stability of PRMT5 to 64°C and inhibited its degradation at 61°C.
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | T1/2 | Tmax | Vz | Cmax | C0 | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 448.373 μg/L·h | 449.564 μg/L·h | 0.879 h | 0.923 h | 2.02 h | 0.125 h | 13.523 L/kg | 593.75 μg/L | 803.704 μg/L | / |
| Rat[1] | 20 mg/kg | p.o. | 1460.7 μg/L·h | 1479.9 μg/L·h | 3.241 h | 3.408 h | 1.827 h | 1.375 h | 44.385 L/kg | 347.75 μg/L | / | 35.2 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mouse (female, 4-6 weeks old, subcutaneous injection of 5×106 MDA-MB-231 cells)[1]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 28 days
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Result:Achieved a tumor growth inhibition and reduced tumor volume.\n
Induced dose-dependent reduction in tumor tissue SDMA protein expression.
Increased cleaved-caspase 3 and cPARP protein expression in tumor tissue.\n
Reduced tumor tissue PARP1 protein expression.\n
Maintained normal mouse physical activity.
Chemical Information
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CAS No. 3105952-57-3
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Molecular Weight 441.28
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Formula C19H17BrN6O2
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SMILES
CON(CC1=CC=C(C=N1)Br)C(C2=CC=C(C3=C2)N=C(C4=C3N(N=C4)C)N)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PRMT5-MTA-IN-8 Related Classifications
HY-181260 Related Classifications
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