JAK1/2 ligand 1
Based on 1 Customer Validation
JAK1/2 ligand 1 is a ligand for the PROTAC target protein of JAK1/2, which can be used to synthesize PROTAC JAK1/2 degrader-1 (HY-179715). JAK1/2 ligand 1 is applicable to the research of colitis.
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- Purity: 99.91%
- CAS No.: 1026028-96-5
- 화학식: C17H13N3O2
- 분자량:291.30
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보관:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Biological Activity
|
JAK1 |
JAK2 |
JAK1/2 ligand 1 (compound 8b) (1.5 μM) does not induce JAK1 degradation in LPS-stimulated Raw 264.7 cells, either alone or in combination with Pomalidomide (HY-10984)[1].
JAK1/2 ligand 1 (0.469-60 μM; 24 h) exhibits a favorable cellular safety profile in LPS-stimulated Raw 264.7 cells, showing no significant cytotoxicity within the tested concentration range[1].
JAK1/2 ligand 1 (0.469-60 μM; 24 h) exhibits only weak inhibitory activity against LPS-induced NO production[1].
AK1/2 ligand 1 (0.94-60 μM; 24 h) promotes JAK2 degradation in LPS-stimulated RAW 264.7 cells[1].
JAK1/2 ligand 1 (0.05-60 μM; 24 h) shows weaker inhibitory activity against LPS-induced TNF-α and IL-6 secretion[1].
JAK1/2 ligand 1 (0.029-3.75 μM; 24 h) suppresses LPS-induced NO, IL-6, and TNF-α production in a dose-dependent manner in Raw 264.7 cells and is non-cytotoxic at concentrations up to 3.75 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-stimulated Raw 264.7 cells
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Concentration:0.469-60 μM
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Incubation Time:24 h
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Result:Showed no significant cytotoxicity at concentrations up to 60 μM.
Exhibited only weak inhibitory activity against LPS-induced NO production.
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Cell Line:LPS-stimulated Raw 264.7 cells
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Concentration:0.94-60 μM
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Incubation Time:24 h
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Result:Caused a concentration-dependent decrease in JAK2 protein levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male/female not specified; DSS-induced colitis model)[1]
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Dosage:40 mg/kg
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Administration:p.o.; daily; 7 days
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Result:Exerted mild protective effects on weight loss, disease activity index progression, and colon length shortening.
Showed minimal improvement in mucosal injury, goblet cell restoration, and inflammation reduction.
Produced a smaller decrease in IL-6, IL-1β, and TNF-α levels and a smaller increase in IL-10 levels compared to compound A8.
Chemical Information
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CAS No. 1026028-96-5
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Appearance Solid
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분자량 291.30
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화학식 C17H13N3O2
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Color Light yellow to yellow
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SMILES
O=C(O)C1=CC=C(C2=NC(NC3=CC=CC=C3)=NC=C2)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
용액&용해도
DMSO : 25.75 mg/mL (88.40 mM; Need 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, 6 months; -20°C, 1 month (stored under nitrogen). 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 (stored under nitrogen). 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)
순도&문서
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Data Sheet (274 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 (stored under nitrogen). 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 | 3.4329 mL | 17.1644 mL | 34.3289 mL | 85.8222 mL |
| 5 mM | 0.6866 mL | 3.4329 mL | 6.8658 mL | 17.1644 mL | |
| 10 mM | 0.3433 mL | 1.7164 mL | 3.4329 mL | 8.5822 mL | |
| 15 mM | 0.2289 mL | 1.1443 mL | 2.2886 mL | 5.7215 mL | |
| 20 mM | 0.1716 mL | 0.8582 mL | 1.7164 mL | 4.2911 mL | |
| 25 mM | 0.1373 mL | 0.6866 mL | 1.3732 mL | 3.4329 mL | |
| 30 mM | 0.1144 mL | 0.5721 mL | 1.1443 mL | 2.8607 mL | |
| 40 mM | 0.0858 mL | 0.4291 mL | 0.8582 mL | 2.1456 mL | |
| 50 mM | 0.0687 mL | 0.3433 mL | 0.6866 mL | 1.7164 mL | |
| 60 mM | 0.0572 mL | 0.2861 mL | 0.5721 mL | 1.4304 mL | |
| 80 mM | 0.0429 mL | 0.2146 mL | 0.4291 mL | 1.0728 mL |