PRMT5-IN-35
Based on 1 Customer Validation
PRMT5-IN-35 (Compound 87) is a potent, selective and orally active PRMT5 inhibitor with an IC50 value of 1 nM. PRMT5-IN-35 can be used in cancer research.
For research use only. We do not sell to patients.
- Purity: 99.63%
- CAS No.: 1989620-03-2
- Formula: C17H17ClN4O4
- Molecular Weight:376.79
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Histone Methyltransferase Isoforms
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Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
10.8 nM
Compound: 46
|
Antiproliferation activity against human A-375 cells assessed as cell growth inhibition
Antiproliferation activity against human A-375 cells assessed as cell growth inhibition
|
[PMID: 36274274] |
| A-375 | IC50 |
11 nM
Compound: 2
|
Antiproliferative activity against human A375 cells measured after 7 days by cell titer glo-based luminescence assay
Antiproliferative activity against human A375 cells measured after 7 days by cell titer glo-based luminescence assay
|
[PMID: 30956011] |
| A549 | IC50 |
5 nM
Compound: 2
|
Antiproliferative activity against human A549 cells incubated for 7 days with compound replacement on day 4 by cell titer glo-based luminescence assay
Antiproliferative activity against human A549 cells incubated for 7 days with compound replacement on day 4 by cell titer glo-based luminescence assay
|
[PMID: 30956011] |
| Sf21 | IC50 |
1 nM
Compound: 2
|
Inhibition of full length N-terminal FLAG-tagged PRMT5 (unknown origin)/MEP50 (unknown origin) expressed in baculovirus infected Sf21 insect cells using H4(1-21) peptide SGRGKGGKGLGKGGAKRHRKV as substrate measured after 25 minutes in the presence of [3H]S
Inhibition of full length N-terminal FLAG-tagged PRMT5 (unknown origin)/MEP50 (unknown origin) expressed in baculovirus infected Sf21 insect cells using H4(1-21) peptide SGRGKGGKGLGKGGAKRHRKV as substrate measured after 25 minutes in the presence of [3H]S
|
[PMID: 30956011] |
| Sf9 | IC50 |
4.3 nM
Compound: 2
|
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (1 to 637 residue) /full length human N-terminal His tagged MEP50 expressed in baculovirus infected Sf9 insect cells assessed as reduction in methyl transfer from [3H]-SAM to biotinylated histon
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (1 to 637 residue) /full length human N-terminal His tagged MEP50 expressed in baculovirus infected Sf9 insect cells assessed as reduction in methyl transfer from [3H]-SAM to biotinylated histon
|
[PMID: 30956011] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1989620-03-2
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Appearance Solid
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Molecular Weight 376.79
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Formula C17H17ClN4O4
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Color White to off-white
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SMILES
O[C@H]1[C@@H](O)[C@H](N2C3=NC=NC(N)=C3C=C2)O[C@@H]1[C@H](O)C4=CC=C(Cl)C=C4
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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 : 125 mg/mL (331.75 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 (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 2.6540 mL | 13.2700 mL | 26.5400 mL | 66.3500 mL |
| 5 mM | 0.5308 mL | 2.6540 mL | 5.3080 mL | 13.2700 mL | |
| 10 mM | 0.2654 mL | 1.3270 mL | 2.6540 mL | 6.6350 mL | |
| 15 mM | 0.1769 mL | 0.8847 mL | 1.7693 mL | 4.4233 mL | |
| 20 mM | 0.1327 mL | 0.6635 mL | 1.3270 mL | 3.3175 mL | |
| 25 mM | 0.1062 mL | 0.5308 mL | 1.0616 mL | 2.6540 mL | |
| 30 mM | 0.0885 mL | 0.4423 mL | 0.8847 mL | 2.2117 mL | |
| 40 mM | 0.0663 mL | 0.3317 mL | 0.6635 mL | 1.6587 mL | |
| 50 mM | 0.0531 mL | 0.2654 mL | 0.5308 mL | 1.3270 mL | |
| 60 mM | 0.0442 mL | 0.2212 mL | 0.4423 mL | 1.1058 mL | |
| 80 mM | 0.0332 mL | 0.1659 mL | 0.3317 mL | 0.8294 mL | |
| 100 mM | 0.0265 mL | 0.1327 mL | 0.2654 mL | 0.6635 mL |