Cystatin B agonist 1
Cystatin B agonist 1 is an orally active MMP-2/9 inhibitor. Cystatin B agonist 1 exhibits inhibitory effects with IC50 values of 3.95 and 3.43 μM against U87 and T98G cells, respectively. Cystatin B agonist 1 induces the cell-cycle arrest at S phase, inhibits angiogenesis, and suppresses migration and invasion of MG cells. Cystatin B agonist 1 inhibits tumor growth in U87 MG xenograft model. Cystatin B agonist 1 can be used for the study of malignant glioma (MG).
For research use only. We do not sell to patients.
- Formula: C19H20O6
- Molecular Weight:344.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3.2 μM
Compound: 1q
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Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 35090346] |
| NCI-H460 | IC50 |
3 μM
Compound: 1q
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Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human NCI-H460 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 35090346] |
Cystatin B agonist 1 (Compound 1e) (2.5-6 μM, 14 days) inhibits the colony formation of U87 and U251 cells in a concentration-dependent fashion[1].
Cystatin B agonist 1 (2.5-6 μM, 24 h) induces S cycle arrest in U87 and U251 cells[1].
Cystatin B agonist 1(2-6 μM, 6 h) attenuates the tube-forming capacity of both U87 and HUVEC cells[1].
Cystatin B agonist 1 (2.5-6 μM, 6-24 h) inhibits migration and invasion of MG cell lines (U87 and U251 cells)[1].
Cystatin B agonist 1(5-6 μM) increases the expression of E-cadherin and decreases the expression of Vimentin, and matrix metalloproteinases (MMPs) in U87 and U251 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87 and U251 cells
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Concentration:2.5, 3, 5, 6 μM
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Incubation Time:24 h
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Result:Induced S cycle arrest in U87 and U251 cells.
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Cell Line:U87 and U251 cells
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Concentration:2.5, 3, 5, 6 μM
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Incubation Time:24 h
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Result:Inhibited migration in U87 and U251 cells.
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Cell Line:U87 and U251 cells
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Concentration:2.5, 3, 5, 6 μM
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Incubation Time:48 h
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Result:Inhibited invasion in U87 and U251 cells.
| Species | Dose | Route | Cmax | T1/2 | Tmax | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | CL/F |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 100 mg/kg | p.o. | 52.3 ng/mL | 4.9 h | 1.5 h | 236.4 ng·h/mL | 243.8 ng·h/mL | 4.2 h | 5.3 h | 442 L/h/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (18-20 g, 6-8 weeks old) were injected subcutaneously with U87 cells suspended in 100 μL PBS (1 × 107 cells/mL)[1]
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Dosage:50, 100 mg/kg
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Administration:Oral gavage for five consecutive days and two-day intervals for 3 weeks
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Result:Reduced tumor growth.
Showed no significant changes in body weight.
Decreased the levels of Ki-67, Vimentin, and MMP2 proteins.
Chemical Information
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Molecular Weight 344.36
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Formula C19H20O6
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SMILES
C=C1C(O[C@H]2CC3=C[C@@H](OC3=O)C/C(C)=C/[C@H]([C@H]12)OC(C4CC4)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cystatin B agonist 1 Related Classifications
HY-175291 Related Classifications
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