PRMT5-IN-30
Based on 1 Customer Validation
PRMT5-IN-30 (compound 17) is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.33 μM and a Kd of 0.987 μM. PRMT5-IN-30 exhibits a broad selectivity against a panel of other methyltransferases. PRMT5-IN-30 inhibits PRMT5 mediated SmD3 methylation.
For research use only. We do not sell to patients.
- Purity: 99.35%
- CAS No.: 330951-01-4
- Formula: C18H17N3O4S
- Molecular Weight:371.41
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
More
Biological Activity
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PRMT5 0.33 μM (IC50) |
PRMT5 0.987 μM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>100 μM
Compound: 17
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Inhibition of recombinant human N-terminal FLAG-tagged PRMT4 (2 to end residues) expressed in HEK293F cells using of histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl methionine addition measured after 60 mins by alpha LISA
Inhibition of recombinant human N-terminal FLAG-tagged PRMT4 (2 to end residues) expressed in HEK293F cells using of histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl methionine addition measured after 60 mins by alpha LISA
|
[PMID: 28650658] |
| HEK293 | IC50 |
0.33 μM
Compound: 17
|
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells using histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl meth
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells using histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl meth
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[PMID: 28650658] |
| JeKo-1 | EC50 |
15 μM
Compound: 17
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Cytotoxicity against human JeKo1 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
Cytotoxicity against human JeKo1 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
|
[PMID: 28650658] |
| KOPN-8 | EC50 |
15 μM
Compound: 17
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Cytotoxicity against human KOPN8 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay
Cytotoxicity against human KOPN8 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay
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[PMID: 28650658] |
| MV4-11 | EC50 |
25.73 μM
Compound: 17
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Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay
Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 8 days by Cell Titer-Glo assay
|
[PMID: 28650658] |
| MV4-11 | EC50 |
6.53 μM
Compound: 17
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Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
|
[PMID: 28650658] |
| MV4-11 | EC50 |
80.74 μM
Compound: 17
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Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 4 days by Cell Titer-Glo assay
Cytotoxicity against human MV411 cells assessed as cell growth inhibition after 4 days by Cell Titer-Glo assay
|
[PMID: 28650658] |
| Z-138 | EC50 |
15 μM
Compound: 17
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Cytotoxicity against human Z138 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
Cytotoxicity against human Z138 cells assessed as cell growth inhibition after 12 days by Cell Titer-Glo assay
|
[PMID: 28650658] |
Chemical Information
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CAS No. 330951-01-4
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Appearance Solid
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Molecular Weight 371.41
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Formula C18H17N3O4S
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Color White to off-white
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SMILES
C1(SCC(=O)NC2C=CC=CC=2C(OC)=O)NC2C(=CC=C(OC)C=2)N=1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (134.62 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. 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. 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 (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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. 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 | 2.6924 mL | 13.4622 mL | 26.9244 mL | 67.3111 mL |
| 5 mM | 0.5385 mL | 2.6924 mL | 5.3849 mL | 13.4622 mL | |
| 10 mM | 0.2692 mL | 1.3462 mL | 2.6924 mL | 6.7311 mL | |
| 15 mM | 0.1795 mL | 0.8975 mL | 1.7950 mL | 4.4874 mL | |
| 20 mM | 0.1346 mL | 0.6731 mL | 1.3462 mL | 3.3656 mL | |
| 25 mM | 0.1077 mL | 0.5385 mL | 1.0770 mL | 2.6924 mL | |
| 30 mM | 0.0897 mL | 0.4487 mL | 0.8975 mL | 2.2437 mL | |
| 40 mM | 0.0673 mL | 0.3366 mL | 0.6731 mL | 1.6828 mL | |
| 50 mM | 0.0538 mL | 0.2692 mL | 0.5385 mL | 1.3462 mL | |
| 60 mM | 0.0449 mL | 0.2244 mL | 0.4487 mL | 1.1219 mL | |
| 80 mM | 0.0337 mL | 0.1683 mL | 0.3366 mL | 0.8414 mL | |
| 100 mM | 0.0269 mL | 0.1346 mL | 0.2692 mL | 0.6731 mL |
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