2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation JAK/STAT Signaling Stem Cell/Wnt MAPK/ERK Pathway Apoptosis Cell Cycle/DNA Damage
  3. Glycosidase NF-κB COX STAT ERK p38 MAPK Apoptosis CDK Survivin Bcl-2 Family
  4. G721-0282

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 research on neuroinflammatory conditions and cancer.

For research use only. We do not sell to patients.

G721-0282 Chemical Structure

G721-0282 Chemical Structure

CAS No. : 946378-12-7

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G721-0282 Related Antibodies

Top Publications Citing Use of Products

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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COX COX-1 COX-2 COX-3

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STAT3 STAT5 STAT6 STAT1

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ERK ERK1 ERK2 ERK5 ERK8

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

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Description

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 research on neuroinflammatory conditions and cancer[1][2].

IC50 & Target

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.

G721-0282 Related Antibodies

Western Blot Analysis[2]

Cell Line: MG63 and U2OS cells
Concentration: 10, 30 and 50 μM
Incubation Time: 24 h
Result: Significantly reduced the level of Cyclin D1, cdk4, cdk6, ERK1/2, JNK, p38, Src, STAT3, Survivin, and Bcl-2 and increased the level 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.
Molecular Weight

376.47

Formula

C18H24N4O3S
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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G721-0282 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

G721-0282946378-12-7GlycosidaseNF-κBCOXSTATERKp38 MAPKApoptosisCDKSurvivinBcl-2 FamilyNuclear factor-κBNuclear factor-kappaBCyclooxygenaseExtracellular signal regulated kinasesCyclin dependent kinaseCHI3L1neuroinflammationanxietyCUMScancerapoptosisSTAT3MAPKInhibitorinhibitorinhibit

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