YN11
YN11 is a STAT3 inhibitor (Kd=11.9 μM). YN11 directly binds to the SH2 domain of STAT3, inhibits the phosphorylation of STAT3, and reduces the expression of downstream target proteins. YN11 induces cell cycle arrest, promotes apoptosis, and inhibits cell invasion and migration in prostate cancer cells. YN11 suppresses tumor growth in a prostate cancer xenograft mouse model. YN11 does not cause significant body weight loss or obvious histopathological changes in major organs in xenograft mice. YN11 is applicable to relevant research on prostate cancer.
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- CAS No.: 3118507-43-7
- Formule: C25H22N2O8S
- Masse moléculaire:510.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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STAT3 11.9 μM (Ki) |
YN11 (24 h) strongly suppresses STAT3-mediated transcriptional activity in IL-6-stimulated HEK293T cells with an IC50 of 0.17 μM[1].
YN11 (72 h) potently inhibits the proliferation of DU145 and 22RV1 prostate cancer cells with IC50 values of 23 nM and 389 nM, respectively, and shows high selectivity for cancer cells over normal BEAS-2B cells with an SI of 82[1].
YN11 (0.01-0.1 μM (DU145), 0.1-1 μM (22RV1); 24 h) dose-dependently inhibits STAT3 phosphorylation in DU145 and 22RV1 prostate cancer cells without altering total STAT3 levels, and downregulates downstream STAT3 target proteins Bcl-2 and Cyclin D1, while showing specificity for STAT3 over STAT1 and STAT5[1].
YN11 (0.01-0.1 μM (DU145), 0.1-1 μM (22RV1); 24 h) induces S-phase cell cycle arrest in DU145 prostate cancer cells and G2/M-phase cell cycle arrest in 22RV1 prostate cancer cells in a dose-dependent manner after 24 h of incubation[1].
YN11 (0.01-0.1 μM (DU145), 0.1-1 μM (22RV1); 24 h initial treatment, 24 h invasion incubation) dose-dependently inhibits the invasion of DU145 and 22RV1 prostate cancer cells after 24 h of initial treatment and a subsequent 24 h invasion incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DU145 and 22RV1 prostate cancer cells
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Concentration:0.01-0.1 μM (DU145 cells); 0.1-1 μM (22RV1 cells)
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Incubation Time:24 h
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Result:Reduced the level of phosphorylated STAT3 (p-STAT3) in a dose-dependent manner in both DU145 and 22RV1 cells, without affecting total STAT3 protein levels.
Reduced the levels of downstream target proteins Bcl-2 and Cyclin D1 in a dose-dependent manner in both cell lines.
Did not affect expression or phosphorylation of STAT1 or STAT5.
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Cell Line:DU145 and 22RV1 prostate cancer cells
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Concentration:0.01-0.1 μM (DU145 cells); 0.1-1 μM (22RV1 cells)
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Incubation Time:24 h
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Result:Induced apoptosis in a dose-dependent manner in both cell lines.
0.1 μM YN11 increased DU145 cell apoptosis to 29.11%.
1 μM YN11 increased 22RV1 cell apoptosis to 31.94%.
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Cell Line:DU145 and 22RV1 prostate cancer cells
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Concentration:0.01-0.1 μM (DU145 cells); 0.1-1 μM (22RV1 cells)
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Incubation Time:24 h
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Result:Induced S-phase cell cycle arrest in a dose-dependent manner in DU145 cells, with 0.1 μM increasing the proportion of S-phase cells to 28.68%.
Induced G2/M-phase cell cycle arrest in a dose-dependent manner in 22RV1 cells, with 1 μM increasing the proportion of G2/M-phase cells to 33.33%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice with Prostate cancer (male, 5 weeks old, subcutaneous xenograft model)[1]
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Dosage:20 mg/kg
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Administration:i.p.; once every other day; 17 days
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Result:Reduced relative tumor volume and tumor weight, resulting in a tumor growth inhibition (TGI) rate of 50.60%.
Significantly suppressed STAT3 phosphorylation, and reduced Bcl-2 and Cyclin D1 expression in tumor tissues.
Caused no body weight loss, and histopathological analysis of major organs (liver, heart, kidney, lung, spleen) showed no observable pathological injuries.
Chemical Information
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CAS No. 3118507-43-7
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Masse moléculaire 510.52
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Formule C25H22N2O8S
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SMILES
O=C(C1=C2OC(C(N3CCN(S(=O)(C4=CC=C(OC)C(OC)=C4)=O)CC3)=O)=C1)C5=C(C2=O)C=CC=C5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YN11 Related Classifications
HY-182288 Related Classifications
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