Cystatin B agonist 1

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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 Estructura química

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Descripciòn

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	3.2 3 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 3 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.

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	C_max	T_1/2	T_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	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.

Peso molecular

344.36

Fòrmula

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Ren H, et al. Bioactive sesquiterpene lactones from Elephantopus scaber: semi-synthesis, target fishing, anti-malignant glioma efficacy in vitro and in vivo. Eur J Med Chem. 2025 Nov 5;297:117954. [Content Brief]