G721-0282
Based on 1 Customer Validation
G721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro-apoptotic protein levels and downregulating anti-apoptotic protein levels. G721-0282 can be used for researches on neuroinflammatory conditions and cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.96%
- No. CAS: 946378-12-7
- Fòrmula: C18H24N4O3S
- Peso molecular:376.47
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
CDK4 |
CDK6 |
COX-2 |
Bcl-2 |
p38 |
ERK |
p-STAT3 |
NF-κB |
In Vitro
G721-0282 (5-20 μM) can inhibit Lipopolysaccharides LPS (HY-D1056) induced neuroinflammation in BV-2 cells, including the generation of NO, expression of pro-inflammatory cytokines, and levels of inflammatory proteins[1].
G721-0282 (20 μM) relies on CHI3L1 to exert anti-inflammatory effects in BV-2 cells[1].
G721-0282 (10-50 μM, 24-72 h) inhibits the proliferation of MG63 and U2OS cells in a dose-dependent and time-dependent manner[2].
G721-0282 (0-50 μM, 24 h) can block the cell cycle and induce cell apoptosis in MG63 and U2OS cells by downregulating anti apoptotic proteins levels and upregulating pro apoptotic proteins levels[2].
G721-0282 (0-50 μM, 12-48 h) significantly inhibits the migration and invasion ability in MG63 and U2OS cells by suppressing the STAT3 signaling pathway[2].
G721-0282 (2-4 weeks) inhibits the colony forming ability of Osteosarcoma (OS) cells in soft agar[2].
G721-0282 (0-50 μM, 24 h) reduces the levels of MMP2 and MMP9[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MG63 and U2OS cells
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Concentration:10, 30 and 50 μM
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Incubation Time:24 h
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Result:Significantly reduced the levels of Cyclin D1, cdk4, cdk6, ERK1/2, JNK, p38, Src, STAT3, Survivin, and Bcl-2 and increased the levels of cleaved PARP and Cleaved caspase-3.
In Vivo
G721-0282 (18.9 mg/kg; i.p.; two times a week; for 35 days) has significant anti-tumor activity in the male BALB/c athymic nude mice bearing MG63 tumors[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CUMS-induced male BALB/c mice (8 weeks)[1]
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Dosage:2.5 and 5 mg/kg
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Administration:Oral administration (p.o.); twice a week for 4 weeks
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Result:Significantly reduced anxiety behavior in mice.
Significantly reduced the expression of inflammatory proteins, including iNOS, COX-2, IBA-1, p65, p50 and p-IκBα.
Reduced the expression of inflammatory factors, including TNF-α, IL-1β, and IL-6.
Inhibited the NF-κB signaling pathway.
Decreased the expression of CHI3L1 and IGFBP3 induced by CUMS.
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Animal Model:1×108 MG63 cells injected male BALB/c athymic nude mice (6 weeks)[2]
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Dosage:18.9 mg/kg
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Administration:Intraperitoneal injection (i.p.); two times a week for 35 days
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Result:Significantly inhibited tumor volume and weight.
Reduced the expression of CHI3L1, PCNA, Cyclin D1, and p-STAT3 in tumor tissue.
- RNA extraction experimental
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- Research Protocol for Inflammation-related Diseases
- Research Protocol for Neurological Diseases
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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No. CAS 946378-12-7
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Appearance Solid
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Peso molecular 376.47
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Fòrmula C18H24N4O3S
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Color White to off-white
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SMILES
O=C1C2=C(C(CCCC)=CN=C2N(C)C(N1C)=O)SCC(NCC=C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 5.83 mg/mL (15.49 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)
Pureza y Documentación
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Ficha de datos (279 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ham HJ, et al. G721-0282 Exerts Anxiolytic-Like Effects on Chronic Unpredictable Mild Stress in Mice Through Inhibition of Chitinase-3-Like 1-Mediated Neuroinflammation. Front Cell Neurosci. 2022 Mar 7;16:793835 [Content Brief]
[2]. Park KR, et al. G721-0282 inhibits cell growth and induces apoptosis in human osteosarcoma through down-regulation of the STAT3 pathway. Int J Biol Sci. 2020 Jan 1;16(2):330-341. [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. 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 | 2.6563 mL | 13.2813 mL | 26.5625 mL | 66.4064 mL |
| 5 mM | 0.5313 mL | 2.6563 mL | 5.3125 mL | 13.2813 mL | |
| 10 mM | 0.2656 mL | 1.3281 mL | 2.6563 mL | 6.6406 mL | |
| 15 mM | 0.1771 mL | 0.8854 mL | 1.7708 mL | 4.4271 mL |
G721-0282 Related Classifications
HY-171656 Related Classifications
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