2. Metabolic Enzyme/Protease Cytoskeleton
  3. MMP Cadherin
  4. 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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Cystatin B agonist 1 Related Antibodies

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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].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
3.2 μM
Compound: 1q
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
[PMID: 35090346]
NCI-H460 IC50
3 μM
Compound: 1q
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
[PMID: 35090346]
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.

Cystatin B agonist 1 Related Antibodies

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.
Parmacokinetics
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
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
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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Cystatin B agonist 1 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:

Cystatin B agonist 1Cystatin B agonist1Cystatin B agonist-1MMPCadherinMatrix metalloproteinasesMMP-2/9malignant gliomaU87 cellsT98G cellsInhibitorinhibitorinhibit

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