GSK-5959
Based on 1 Customer Validation
GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM.
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- Pureté: 99.73%
- CAS No.: 901245-65-6
- Formule: C22H26N4O3
- Masse moléculaire:394.47
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
IC50: 80 nM (BRPF1)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.98 μM
Compound: 3
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Binding affinity to NanoLuc-tagged BRPF1 isoform 1 bromodomain (625-735 aa) (unknown origin) expressed in HEK293 cells co-transfected with histone H3.3-HaloTag after 18 hrs by NanoBRET assay
Binding affinity to NanoLuc-tagged BRPF1 isoform 1 bromodomain (625-735 aa) (unknown origin) expressed in HEK293 cells co-transfected with histone H3.3-HaloTag after 18 hrs by NanoBRET assay
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[PMID: 25408830] |
GSK-5959 (3a) also displays selectivity over the closely related family members, BRPF2 (100-fold) and BRPF3 (>1000-fold)[2].
GSK-5959 (3a) exhibits an EC50 = 0.98 μM) in cellular NanoBRET assay[2].
GSK-5959 has no effect on TRIM24 SUMOylation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 901245-65-6
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Appearance Solid
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Masse moléculaire 394.47
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Formule C22H26N4O3
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Color Light yellow to yellow
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SMILES
O=C(NC1=C(N2CCCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 13 mg/mL (32.96 mM; Need ultrasonic and warming; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (583 KB)
- English - EN (583 KB)
- Français - FR (583 KB)
- Deutsch - DE (583 KB)
- Norwegian - NO (583 KB)
- Español - ES (583 KB)
- Swedish - SV (583 KB)
- Italian - IT (583 KB)
- Korean - KR (583 KB)
- Portuguese - PT (583 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Demont EH, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. (2014) ACS Med Chem Lett. 5(11):1190-1195. [Content Brief]
[3]. Srikanth Appikonda, et al. Cross-talk between chromatin acetylation and SUMOylation of tripartite motif-containing protein 24 (TRIM24) impacts cell adhesionJ Biol Chem. 2018 May 11;293(19):7476-7485. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5350 mL | 12.6752 mL | 25.3505 mL | 63.3762 mL |
| 5 mM | 0.5070 mL | 2.5350 mL | 5.0701 mL | 12.6752 mL | |
| 10 mM | 0.2535 mL | 1.2675 mL | 2.5350 mL | 6.3376 mL | |
| 15 mM | 0.1690 mL | 0.8450 mL | 1.6900 mL | 4.2251 mL | |
| 20 mM | 0.1268 mL | 0.6338 mL | 1.2675 mL | 3.1688 mL | |
| 25 mM | 0.1014 mL | 0.5070 mL | 1.0140 mL | 2.5350 mL | |
| 30 mM | 0.0845 mL | 0.4225 mL | 0.8450 mL | 2.1125 mL |
GSK-5959 Related Classifications
HY-18665 Related Classifications
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