PRMT5-IN-1
PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
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- CAS No.: 2366149-83-7
- Formule: C19H19ClN4O5
- Masse moléculaire:418.83
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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PRMT5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Granta-519 | IC50 |
0.012 μM
Compound: 9
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Inhibition of PRMT5 in human Granta-519 assessed as reduction in sDMA production incubated for 3 days by Western blotting analysis
Inhibition of PRMT5 in human Granta-519 assessed as reduction in sDMA production incubated for 3 days by Western blotting analysis
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[PMID: 31312404] |
| Granta-519 | IC50 |
0.06 μM
Compound: 9
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Antiproliferative activity against human GRANTA-519 cells assessed as reduction in cell viability supplemented with fresh medium containing compound every 3 days incubated for 10 days by CCK-8 assay
Antiproliferative activity against human GRANTA-519 cells assessed as reduction in cell viability supplemented with fresh medium containing compound every 3 days incubated for 10 days by CCK-8 assay
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[PMID: 31312404] |
PRMT5 IN-1 (0-500 nM) inhibits the PRMT5/MEP50 complex [Kinact/KI=1.2×105 M-1 min-1] very rapidly with a Kinact of 0.068 min-1 and a good binding affinity (KI=55 nM)[1].
PRMT5 IN-1 (0-1000 nM; 3 d; Granta-519 cells) inhibits the expression of cellular sDMA with an IC50 value of 0.012 μM[1].
PRMT5 IN-1 (0-1 μM; 10 d; Granta-519 cells) inhibits cell proliferation in a dose-dependent manner with an IC50 value of 0.06 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Granta-519 cells
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Concentration:0, 0.0001524, 0.000457, 0.001372, 0.004115, 0.012346, 0.037037, 0.111111, 0.333333 and 1 μM
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Incubation Time:10 days
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Result:Inhibited cell proliferative, in which cells died on day 10 at high concentrations (0.3 and 1 μM).
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Cell Line:Granta-519 cells
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Concentration:0, 0.05, 0.15, 0.46, 1.37, 4, 12, 37, 111, 333, 1000 nM
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Incubation Time:3 days
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Result:Inhibited cellular sDMA in Granta-519 cells in a dose-dependent manner.
Chemical Information
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CAS No. 2366149-83-7
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Masse moléculaire 418.83
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Formule C19H19ClN4O5
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SMILES
O[C@@H]1[C@@H]([C@@H](C2=CC=C(Cl)C=C2)O)O[C@@H](N3C=CC4=C3N=CN5C4=NCC5O)[C@@H]1O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PRMT5-IN-1 Related Classifications
HY-126256 Related Classifications
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