1. Metabolic Enzyme/Protease Cytoskeleton
  2. MMP Cadherin
  3. 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).

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Cystatin B agonist 1

Cystatin B agonist 1 Chemical Structure

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Description

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)[1].

In Vitro

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.

Cell Cycle Analysis[1]

Cell Line: U87 and U251 cells
Concentration: 2.5, 3, 5, 6 μM
Incubation Time: 24 h
Result: Induced S cycle arrest in U87 and U251 cells.

Cell Migration Assay [1]

Cell Line: U87 and U251 cells
Concentration: 2.5, 3, 5, 6 μM
Incubation Time: 24 h
Result: Inhibited migration in U87 and U251 cells.

Cell Invasion Assay[1]

Cell Line: U87 and U251 cells
Concentration: 2.5, 3, 5, 6 μM
Incubation Time: 48 h
Result: Inhibited invasion in U87 and U251 cells.
In Vivo

Cystatin B agonist 1 (Compound 1e) (50-100 mg/kg, i.g., five consecutive days and two-day intervals, 21 days) demonstrates excellent anti-tumor efficacy in U87 MG xenograft model [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 50,100 mg/kg
Administration: Oral gavage for five consecutive days and two-day intervals for 3 weeks
Result: Reduced tumor growth.
Showed no significant changes in body weight.
Decreased the levels of Ki-67, Vimentin, and MMP2 proteins.
Molecular Weight

344.36

Formula

C19H20O6

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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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • 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.

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Product Name:
Cystatin B agonist 1
Cat. No.:
HY-175291
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