AH-26
AH-26 is a STAT3 inhibitor. AH-26 stabilizes the STAT3 protein, inhibits STAT3 phosphorylation, induces mitochondria-mediated apoptosis, triggers differentiation of leukemia cells, suppresses cancer cell migration, and arrests the cell cycle at the G1 phase. AH-26 exhibits antitumor activity without toxicity in nude mice. AH-26 can be used in the research of leukemia, ovarian cancer, gastric cancer, and pancreatic cancer.
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- No. CAS: 3083249-46-8
- Fòrmula: C21H23NO4
- Peso molecular:353.41
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Almacenamiento:
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Actividad biológica
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STAT3 |
AH-26 (0.1-20 μM; 72 h) potently inhibits the proliferation of NB4, K562, HL-60, U937, SKOV3, HGC-27, MKN45 and PANC-1 cancer cells, with corresponding IC50 values of 0.16, 0.42, 0.21, 0.36, 0.04, 0.01, 0.49 and 0.10 μM, respectively; meanwhile, it shows low cytotoxicity against normal HK-2 cells[1].
AH-26 (0.1-0.4 μM; 48 h) inhibits the proliferation of SKOV3 and HL-60 cells in a dose-dependent manner[1].
AH-26 (0.05-0.4 μM; 6-12 h) inhibits the migration of SKOV3 and HGC-27 cells in a dose-dependent and time-dependent manner[1].
AH-26 (0.025-0.075 μM; 72 h) upregulates the expression of differentiation markers CD11b and CD14 in NB4 and HL-60 leukemia cells in a dose-dependent manner, and induces cell differentiation[1].
AH-26 (0.05-0.4 μM; 48 h) downregulates Bcl-2, Bcl-XL, c-Myc, pro-caspase-3 and p-STAT3 and upregulates cleaved caspase-3 in SKOV3 cells at concentrations of 0.1-0.4 μM. At concentrations of 0.05-0.1 μM, it downregulates Bcl-2, Bcl-XL, c-Myc, pro-caspase-9 and p-STAT3 and upregulates cleaved caspase-9 in HGC-27 cells, with no significant effect on total STAT3 levels[1].
AH-26 (0.05-0.2 μM; 48 h) induces apoptosis in NB4, K562, HL-60, U937, SKOV3 and HGC-27 cells in a dose-dependent manner[1].
AH-26 (0.05-0.2 μM; 48 h) reduces the mitochondrial membrane potential of NB4, K562, HL-60, U937, SKOV3 and HGC-27 cells in a dose-dependent manner, and triggers mitochondria-mediated apoptosis[1].
AH-26 (0.025-0.5 μM; 48 h) arrests the cell cycle of NB4, HL-60, SKOV3 and HGC-27 cells at the G1 phase in a dose-dependent manner[1].
AH-26 (0.1-0.4 μM; 48 h) increases intracellular ROS levels in HL-60 cells in a dose-dependent manner, and this effect is inhibited by the antioxidant NAC[1].
AH-26 (10 μM; 1 h) increases the thermal stability of STAT3 in SKOV3 and HL-60 cell lysates at 40-49 °C in CETSA, supporting the intracellular interaction between AH-26 and STAT3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKOV3, HL-60 cancer cell lines
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Concentration:0.1, 0.2, 0.4 μM
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Incubation Time:48 h
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Result:Decreased the number of EdU-positive cells significantly in a dose-dependent manner.
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Cell Line:NB4, K562, HL-60, U937, SKOV3, HGC-27 cancer cell lines
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Concentration:0.05-0.2 μM (NB4, K562, HL-60, U937); 0.25-1 μM (HGC-27); 0.05-0.5 μM (SKOV3)
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Incubation Time:48 h
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Result:Showed dense, dark nuclei indicative of apoptosis via Hoechst staining.
Revealed increased apoptotic cells in a dose-dependent manner across all tested cell lines via Annexin V/PI staining.
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Cell Line:NB4, HL-60, SKOV3, HGC-27 cancer cell lines
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Concentration:0.1-0.5 μM (NB4, HGC-27); 0.025-0.075 μM (HL-60, SKOV3)
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Incubation Time:48 h
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Result:Increased the proportion of cells in the G1 phase in a dose-dependent manner, indicating cell cycle arrest at the G1 phase.
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Cell Line:NB4, HL-60 leukemia cell lines
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Concentration:0.025-0.075 μM
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Incubation Time:72 h
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Result:Increased the expression of CD11b and CD14 in a dose-dependent manner, indicating induced differentiation of leukemia cells.
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Cell Line:SKOV3, HGC-27, NB4, HL-60 cancer cell lines
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Concentration:0.1-0.4 μM (SKOV3); 0.05-0.1 μM (HGC-27, NB4); 0.075-0.25 μM (HL-60)
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Incubation Time:48 h
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Result:Downregulated the expression of anti-apoptotic/proliferative proteins (Bcl-2, Bcl-XL, c-Myc, YAP1, XIAP, MCL-1, pro-Caspase 3/9, p-STAT3).
Upregulated the expression of pro-apoptotic activated Caspase 3/9.
Left total STAT3 expression unchanged.
AH-26 (13-26 mg/kg; i.p.; daily administration; 22 days) inhibits the tumor growth of subcutaneous HGC-27 xenografts in nude mice, reduces tumor weight, causes no significant body weight loss or obvious pathological abnormalities in the heart, liver, spleen, lung and kidney, and decreases Ki67 expression in tumor tissues.[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice bearing subcutaneous NB4 xenografts[1]
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Dosage:13 mg/kg; 26 mg/kg
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Administration:i.p.; daily
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Result:Effectively inhibited NB4 tumor growth in vivo.
Significantly reduced tumor weights compared to blank and positive control groups.
Did not cause noticeable mouse body weight decrease.
Showed no prominent macroscopic toxic effects in heart, liver, spleen, lung, and kidney via H&E staining.
Strongly inhibited tumor cell proliferation in vivo via Ki67 staining.
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Animal Model:Nude mice bearing subcutaneous HGC-27 xenografts[1]
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Dosage:13 mg/kg; 26 mg/kg
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Administration:i.p.; daily
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Result:Effectively inhibited HGC-27 tumor growth in vivo.
Significantly reduced tumor weights compared to blank and positive control groups.
Supported consistent mouse body weight increase, unlike blank group.
Showed no prominent macroscopic toxic effects in heart, liver, spleen, lung, and kidney via H&E staining.
Strongly inhibited tumor cell proliferation in vivo via Ki67 staining.
Chemical Information
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No. CAS 3083249-46-8
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Peso molecular 353.41
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Fòrmula C21H23NO4
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SMILES
O=C(O1)C=C2[C@@]13[C@@](CCCC4)([H])N4[C@](C3)([H])C(C5=CC(OC)=CC(OC)=C5)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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