Art. -Nr.: HY-171656

G721-0282

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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.

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Reinheit: 99.96%
CAS. Nr.: 946378-12-7
Formel: C₁₈H₂₄N₄O₃S
Molecular Weight:376.47

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

G721-0282 Chemical Structure

CAS. Nr.: 946378-12-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK4

CDK6

COX-2

Bcl-2

p38

ERK

p-STAT3

NF-κB

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle COX Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

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.

Western Blot Analysis^[2]

Cell Line:

MG63 and U2OS cells
Concentration:

10, 30 and 50 μM
Incubation Time:

24 h
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 (2.5 and 5 mg/kg; p.o.; twice a week; for 4 weeks) significantly reduces anxiety like behavior induced by chronic unpredictable mild stress (CUMS) and inhibits neuroinflammation in male BALB/c mice ^[1].
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.

Animal Model:

CUMS-induced male BALB/c mice (8 weeks)^[1]
Dosage:

2.5 and 5 mg/kg
Administration:

Oral administration (p.o.); twice a week for 4 weeks
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.

Animal Model:

1×10⁸ MG63 cells injected male BALB/c athymic nude mice (6 weeks)^[2]
Dosage:

18.9 mg/kg
Administration:

Intraperitoneal injection (i.p.); two times a week for 35 days
Result:

Significantly inhibited tumor volume and weight.
Reduced the expression of CHI3L1, PCNA, Cyclin D1, and p-STAT3 in tumor tissue.

Chemical Information

CAS. Nr. 946378-12-7
Appearance Solid
Molecular Weight 376.47
Formel C₁₈H₂₄N₄O₃S
Color White to off-white
SMILES

O=C1C2=C(C(CCCC)=CN=C2N(C)C(N1C)=O)SCC(NCC=C)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6563 mL

13.2813 mL

26.5625 mL

5 mM

0.5313 mL

2.6563 mL

5.3125 mL

10 mM

0.2656 mL

1.3281 mL

2.6563 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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G721-0282

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Alle NF-κB Isoform-spezifische Produkte anzeigen

Alle COX Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Alle ERK Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

G721-0282 Related Classifications

HY-171656 Related Classifications