PRMT5-IN-19
PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research.
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- CAS 番号: 2783961-86-2
- 分子式: C25H24N4O
- 分子量:396.48
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Histone Methyltransferase アイソフォーム固有の製品をすべて表示
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生物活性
|
PRMT5 23.9 nM (IC50) |
PRMT1 3.252 μM (IC50) |
PRMT4 >20 μM (IC50) |
PRMT5-IN-19 (Compound 41, 5 days) has strong anti-proliferative effects against the A375 cell with an IC50 value of 1.36 μM[1].
PRMT5-IN-19 shows higher selectivity for PRMT5 (IC50 value of 23.9 nM) than other histone methyltransferases (PRMT1 and PRMT4), and PKMTS (EZH2, NSD2, MLL1, and MLL4) [1].
PRMT5-IN-19 binds with the SAM-binding pocket in PRMT5[1].
PRMT5-IN-19 (4-5 days) Inhibits proliferation of multiple cancer cell lines (A-375, CHL-1, SNU-423, SNU-449, MDA-MB-231, MDA-MA-453, MV-4-11, MOLM13) with IC50 value ranging from 1.08 to 3.45 μM[1].
PRMT5-IN-19 inhibits arginine symmetrical dimethylation in A375 cells [1].
PRMT5-IN-19 (0-4 μM, 48 h) suppresses A375 cell proliferation by inducing apoptosis in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A-375, CHL-1, SNU-423, SNU-449, MDA-MB-231, MDA-MA-453, MV-4-11, MOLM13
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Concentration:0-10 μM
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Incubation Time:5 days
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Result:Inhibited proliferation of multiple cancer cell lines with IC50 value ranging from 1.08 to 3.45 μM.
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Cell Line:A-375 cells
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Concentration:0.5, 1, 2, 4,8 μM
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Incubation Time:48 h.
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Result:Inhibited arginine symmetrical dimethylation in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A375 cell-derived nude mouse xenograft model[1].
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Dosage:75 mg/kg/d
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Administration:P.o., 19 days
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Result:Had no effect on the body weight, displayed antitumor efficacy with a tumor growth inhibition (TGI) rate of 73% by inhibiting the methyltransferase activity of PRMT5.
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Animal Model:Rats and mice[1].
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Dosage:10 mg/kg for p.o., 3 mg/kg for i.v
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Administration:P.o., i.v. (Pharmacokinetic Analysis)
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Result:Pharmacokinetic parameters for PRMT5-IN-19 in SD Rats and Micea,c [1].
species PRMT5-IN-19 T1/2 (h) Cmax (ng/mL) CL (mL/min/kg) F (%) rat iv (3 mg/kg)/td> 2.58 310 po (10 mg/kg)/td> 7.51 8.22 7.25 po (10 mg/kg)/td> 2.95 27.7 23.7 mouse iv (3 mg/kg)/td> 4.71 153 po (10 mg/kg)/td> 128 --> 
化学情報
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CAS 番号 2783961-86-2
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分子量 396.48
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分子式 C25H24N4O
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SMILES
C[C@H](OC1=CC=C(C2=CC3=C(N=CN=C3N2)C4=CCNCC4)C=C1)C5=CC=CC=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
バッチを選択:純度: 99.98%Assay: 99.98%ee.: 99.98%
参考文献
Calculators
モル濃度計算機Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)= × ×希釈計算機濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
×=×
PRMT5-IN-19 関連分類
製品番号: HY-149005
KeywordsAssay Types -
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