CGK012
Based on 1 Customer Validation
CKG012 is an inhibitor for Wnt/βcatenin signaling pathway. CGK012 inhibits release of HMGB1 and transcription of β-catenin, exhibits attenuating activities against cecal ligation and puncture (CLP)-induced sepsis and multiple myeloma cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.96%
- CAS. Nr.: 2044497-76-7
- Formel: C20H23NO5
- Molecular Weight:357.40
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
CGK012 (0-20 μM) inhibits HMGB1-release by reducing LPS-induced HMGB1 acetylation and SIRT1 expression and suppresses therefore the excessive vascular permeability in HUVECs, decreases the expression of pathogen-associated molecules like TLR2/4 without affecting cellular viability of HUVECs.[1].
CGK012 (0-20 μM) exhibits ameliorates inflammatory response through decreases adhesion and migration of inflammatory immune cells, production of proinflammatory cytokines like IL-6, TNF-α, β, and transcription factors NF-kB and ERK1/2[1].
CGK012 (0-20 μM) promotes β-catenin phosphorylation/degradation and repressed the expression β-catenin-dependent genes, thereby inhibiting the proliferation of multiple myeloma cells RPMI-8226 with an IC50 of 5.08 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVEC
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Concentration:5-100 μM
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Incubation Time:48 h
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Result:Revealed no effects on cell viability.
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Cell Line:HUVECs, HEK293-FL reporter, RPMI-8226
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Concentration:0-20 μM
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Incubation Time:12 h
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Result:Reduced levels of SIRT1 and acetylation of HMGB1, inhibited vascular permeability in HUVECs. Reduced levels of β-catenin in HEK293-FL reporter and RPMI-8226.
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Cell Line:HUVEC
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Concentration:0-20 μM
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Incubation Time:6 h
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Result:Inhibited migration of neutrophils through monolayers of HUVECs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CLP- induced sepsis in C57BL/6 mice[1]
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Dosage:0.26-0.53 mg/kg
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Administration:double doses, 12 or 50 h after surgery.
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Result:Reduced expression of HMGB1 and improved the survival rate.
Chemical Information
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CAS. Nr. 2044497-76-7
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Appearance Solid
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Molecular Weight 357.40
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Formel C20H23NO5
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Color White to off-white
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SMILES
O=C(O[C@H]1CC2=CC(C=CC3=O)=C(O3)C=C2OC1(C)C)NC4CCCC4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
DMSO : ≥ 25 mg/mL (69.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (274 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)
Verweise
[1]. Park YJ, et al., Antiseptic Functions of CGK012 against HMGB1-Mediated Septic Responses. Int J Mol Sci. 2024 Mar 4;25(5):2976. [Content Brief]
[2]. Choi PJ,et al., Anti-proliferative activity of CGK012 against multiple myeloma cells via Wnt/β-catenin signaling attenuation. Leuk Res. 2017 Sep;60:103-108. [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, 6 months; -20°C, 1 month (protect from light). 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 | 2.7980 mL | 13.9899 mL | 27.9799 mL | 69.9496 mL |
| 5 mM | 0.5596 mL | 2.7980 mL | 5.5960 mL | 13.9899 mL | |
| 10 mM | 0.2798 mL | 1.3990 mL | 2.7980 mL | 6.9950 mL | |
| 15 mM | 0.1865 mL | 0.9327 mL | 1.8653 mL | 4.6633 mL | |
| 20 mM | 0.1399 mL | 0.6995 mL | 1.3990 mL | 3.4975 mL | |
| 25 mM | 0.1119 mL | 0.5596 mL | 1.1192 mL | 2.7980 mL | |
| 30 mM | 0.0933 mL | 0.4663 mL | 0.9327 mL | 2.3317 mL | |
| 40 mM | 0.0699 mL | 0.3497 mL | 0.6995 mL | 1.7487 mL | |
| 50 mM | 0.0560 mL | 0.2798 mL | 0.5596 mL | 1.3990 mL | |
| 60 mM | 0.0466 mL | 0.2332 mL | 0.4663 mL | 1.1658 mL |
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