GSK1362
Based on 1 Customer Validation
GSK1362 is a selective inverse agonist of REV-ERB. GSK1362disrupts the interaction of REV-ERBα with repressive co-modulators (NCoR1, SMRT2, RIP140). GSK1362 exerts an inverse agonist effect by increasing the transcription of BMAL1 to relieve BMAL1 repression by endogenous REV-ERB ligands. GSK1362 suppresses LPS (HY-D1056)-induced inflammatory cytokine expression, inhibits IL-1β-induced Cxcl5 transcription in cells. GSK1362 can be used for the study of inflammatory diseases.
For research use only. We do not sell to patients.
- Purity: 96.38%
- CAS No.: 2986733-57-5
- Formula: C21H21ClN4O2
- Molecular Weight:396.87
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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
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Biological Activity
GSK1362 (24 h) increases transcription in a concentration-dependent manner in HEK293 cells cotransfected with HA-Rev-Erbα and Bmal1-Luc reporter, exerting an inverse agonist effect to relieve BMAL1 repression by endogenous REV-ERB ligands like heme[1].
GSK1362 (10 μM, 4 h) inhibits LPS (HY-D1056)-induced production of several inflammatory cytokines in alveolar macrophages collected at ZT8[1].
GSK1362 (10 μM, 16 h) inhibits the induction of Cxcl5 transcription in serum shock-synchronized mouse LA-4 cells[1].
GSK1362 (10 μM, 4 h) significantly increases REV-ERBα protein abundance in serum shock-synchronized human primary bronchial epithelial (NHBE) cells[1].
GSK1362 (10 μM, pretreated for 15 min) stabilizes REV-ERBα protein and counteracts IL-1β-induced REV-ERBα protein degradation in serum shock-synchronized NHBE cells[1].
GSK1362 (10 μM, 4 h) blocks IL-1β or TNF-α-induced ubiquitination of REV-ERBα in HEK293T cells transfected with HA-Rev-Erbα, His-Ub and SENP-1 plasmids[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2986733-57-5
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Appearance Solid
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Molecular Weight 396.87
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Formula C21H21ClN4O2
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Color White to light yellow
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SMILES
N#CC1=C(NCCOC)OC(C2=CC=C(N(CC3=CC=C(C=C3)Cl)C)C=C2)=N1
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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 : 100 mg/mL (251.97 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 | 2.5197 mL | 12.5986 mL | 25.1972 mL | 62.9929 mL |
| 5 mM | 0.5039 mL | 2.5197 mL | 5.0394 mL | 12.5986 mL | |
| 10 mM | 0.2520 mL | 1.2599 mL | 2.5197 mL | 6.2993 mL | |
| 15 mM | 0.1680 mL | 0.8399 mL | 1.6798 mL | 4.1995 mL | |
| 20 mM | 0.1260 mL | 0.6299 mL | 1.2599 mL | 3.1496 mL | |
| 25 mM | 0.1008 mL | 0.5039 mL | 1.0079 mL | 2.5197 mL | |
| 30 mM | 0.0840 mL | 0.4200 mL | 0.8399 mL | 2.0998 mL | |
| 40 mM | 0.0630 mL | 0.3150 mL | 0.6299 mL | 1.5748 mL | |
| 50 mM | 0.0504 mL | 0.2520 mL | 0.5039 mL | 1.2599 mL | |
| 60 mM | 0.0420 mL | 0.2100 mL | 0.4200 mL | 1.0499 mL | |
| 80 mM | 0.0315 mL | 0.1575 mL | 0.3150 mL | 0.7874 mL | |
| 100 mM | 0.0252 mL | 0.1260 mL | 0.2520 mL | 0.6299 mL |
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