PRMT1-IN-3
PRMT1-IN-3 is a potent protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 4.11 μM. PRMT1-IN-3 inhibits PRMT6 and PRMT8 with IC50s of 23.3 and 30.1 μM. PRMT1-IN-3 suppresses asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells. PRMT1-IN-3 induces cell cycle arrest, apoptosis, and inhibits migration and colony formation in MDA-MB-231 cells. PRMT1-IN-3 acts as chemotherapeutic sensitizers for Paclitaxel (HY-B0015). PRMT1-IN-3 can be used for the study of TNBC.
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- CAS No.: 892570-48-8
- 화학식: C18H23FN2O
- 분자량:302.39
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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
More
Biological Activity
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PRMT1 4.11 μM (IC50) |
PRMT3 > 100 μM (IC50) |
PRMT4 > 100 μM (IC50) |
PRMT6 23.3 μM (IC50) |
PRMT5 > 100 μM (IC50) |
PRMT8 30.1 μM (IC50) |
PRMT7 > 100 μM (IC50) |
PRMT1-IN-3 (Compound YH-4) (10 μM, 37-65°C) significantly enhances the thermal stability of PRMT1 (ΔTm = +5.2°C) and has no significant effect on other PRMT subtypes[1].
PRMT1-IN-3 (0.01-100 μM, 48 h) inhibits MDA-MB-231, HCT116, HeLa, and A549 cells growth with IC50s of 6.38 μM, 15.29 μM, 12.97 μM, and 9.187 μM, respectively[1].
PRMT1-IN-3 (1.25-10 μM, 48 h) dose-dependently inhibits ADMA levels and H4R3me2a modification in MDA-MB-231 cells[1].
PRMT1-IN-3 (0-20 μM, 72 h) (resistance ratio: 9.0) shows synergistic effect with Paclitaxel (PTX) (resistance ratio: 92.7) in MDA-MB-231 cells and MDA-MB-231/Taxol cells[1].
PRMT1-IN-3 (0-40 μM, 0-48 h) induces G0/G1 phase arrest and cell apoptosis, and inhibits cell migration in MDA-MB-231 cells[1].
PRMT1-IN-3 (0-20 μM, 10 days) almost completely inhibits MDA-MB-231 cells colony formation at 20 μM[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, 5, 20 and 40 μM
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Incubation Time:48 h
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Result:Resulted in an increase in early apoptosis from 2.34 % to 34.3 % from 2.5 μM to 40 μM.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 2.5, 5, 10, 20 μM
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Incubation Time:48 h
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Result:Observed that the proportion of cells in the G0/G1 phase increased in a dose-dependent manner from 41.8 % to 60.9 %, while the proportions of cells in the S phase and G2/M phase decreased in a dose-dependent manner from 33.2 % to 23.6 % and from 24.9 % to 15.2 %, respectively.
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Cell Line:MDA-MB-231 cells
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Concentration:1.25, 2.5, 5, 10 and 20 μM
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Incubation Time:0, 12, 36, and 48 h
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Result:Decreased the healing rate to 18.52% after 48 h at 20 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA-MB-23-YFP-Luc cells induced xenograft model established in female nude mice 4-5 weeks old weighing 16-18 g[1]
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Dosage:30 mg/kg with or without PTX
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Administration:Intraperitoneal injection (i.p.), for one week, then discontinue for three days, for a total of 21 days
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Result:Demonstrated significant inhibitory effects on tumor volume, with the combination of PTX showing a markedly superior antitumor efficacy compared to the monotherapies.
Chemical Information
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CAS No. 892570-48-8
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분자량 302.39
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화학식 C18H23FN2O
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SMILES
FC1=CC=C(COC2=C(C=CC=C2)CNCCCNC)C=C1
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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)
PRMT1-IN-3 Related Classifications
HY-175821 Related Classifications
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