PRMT5-IN-1 hydrochloride
Based on 1 Customer Validation
PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
For research use only. We do not sell to patients.
- Purity: 99.51%
- Formula: C20H22Cl2N4O5
- Molecular Weight:469.32
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All Histone Methyltransferase Isoforms
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Biological Activity
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PRMT5 |
PRMT5 IN-1 (compound 9; 0-500 nM) hydrochlorideinhibits 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) hydrochloride 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) hydrochloride 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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Appearance Solid
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Molecular Weight 469.32
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Formula C20H22Cl2N4O5
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Color Off-white to pink
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SMILES
O[C@@H]1[C@@H](O)[C@H](N2C=CC3=C2N=CN4C3=NCC4O)O[C@H]1C[C@H](C5=CC=C(Cl)C=C5)O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 125 mg/mL (266.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1307 mL | 10.6537 mL | 21.3074 mL | 53.2686 mL |
| 5 mM | 0.4261 mL | 2.1307 mL | 4.2615 mL | 10.6537 mL | |
| 10 mM | 0.2131 mL | 1.0654 mL | 2.1307 mL | 5.3269 mL | |
| 15 mM | 0.1420 mL | 0.7102 mL | 1.4205 mL | 3.5512 mL | |
| 20 mM | 0.1065 mL | 0.5327 mL | 1.0654 mL | 2.6634 mL | |
| 25 mM | 0.0852 mL | 0.4261 mL | 0.8523 mL | 2.1307 mL | |
| 30 mM | 0.0710 mL | 0.3551 mL | 0.7102 mL | 1.7756 mL | |
| 40 mM | 0.0533 mL | 0.2663 mL | 0.5327 mL | 1.3317 mL | |
| 50 mM | 0.0426 mL | 0.2131 mL | 0.4261 mL | 1.0654 mL | |
| 60 mM | 0.0355 mL | 0.1776 mL | 0.3551 mL | 0.8878 mL | |
| 80 mM | 0.0266 mL | 0.1332 mL | 0.2663 mL | 0.6659 mL | |
| 100 mM | 0.0213 mL | 0.1065 mL | 0.2131 mL | 0.5327 mL |