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Art. -Nr.: HY-184731

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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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CAS. Nr.: 3083249-46-8
Formel: C₂₁H₂₃NO₄
Molecular Weight:353.41

Speicherung:

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

AH-26 Chemical Structure

CAS. Nr.: 3083249-46-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

STAT3

Alle STAT Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Cell Proliferation Assay^[1]

Cell Line:

SKOV3, HL-60 cancer cell lines
Concentration:

0.1, 0.2, 0.4 μM
Incubation Time:

48 h
Result:

Decreased the number of EdU-positive cells significantly in a dose-dependent manner.

Apoptosis Analysis^[1]

Cell Line:

NB4, K562, HL-60, U937, SKOV3, HGC-27 cancer cell lines
Concentration:

0.05-0.2 μM (NB4, K562, HL-60, U937); 0.25-1 μM (HGC-27); 0.05-0.5 μM (SKOV3)
Incubation Time:

48 h
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.

Cell Cycle Analysis^[1]

Cell Line:

NB4, HL-60, SKOV3, HGC-27 cancer cell lines
Concentration:

0.1-0.5 μM (NB4, HGC-27); 0.025-0.075 μM (HL-60, SKOV3)
Incubation Time:

48 h
Result:

Increased the proportion of cells in the G1 phase in a dose-dependent manner, indicating cell cycle arrest at the G1 phase.

Cell Differentiation Assay^[1]

Cell Line:

NB4, HL-60 leukemia cell lines
Concentration:

0.025-0.075 μM
Incubation Time:

72 h
Result:

Increased the expression of CD11b and CD14 in a dose-dependent manner, indicating induced differentiation of leukemia cells.

Western Blot Analysis^[1]

Cell Line:

SKOV3, HGC-27, NB4, HL-60 cancer cell lines
Concentration:

0.1-0.4 μM (SKOV3); 0.05-0.1 μM (HGC-27, NB4); 0.075-0.25 μM (HL-60)
Incubation Time:

48 h
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.

In Vivo

AH-26 (13-26 mg/kg; i.p.; daily administration; 14 days) inhibits tumor growth and reduces tumor weight in nude mice bearing subcutaneous NB4 xenografts, without causing significant body weight loss or obvious pathological abnormalities in the heart, liver, spleen, lung and kidney, and decreases Ki67 expression in tumor tissues^[1].
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.

Animal Model:

Nude mice bearing subcutaneous NB4 xenografts^[1]
Dosage:

13 mg/kg; 26 mg/kg
Administration:

i.p.; daily
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.

Animal Model:

Nude mice bearing subcutaneous HGC-27 xenografts^[1]
Dosage:

13 mg/kg; 26 mg/kg
Administration:

i.p.; daily
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

CAS. Nr. 3083249-46-8
Molecular Weight 353.41
Formel C₂₁H₂₃NO₄
SMILES

O=C(O1)C=C2[C@@]13[C@@](CCCC4)([H])N4[C@](C3)([H])C(C5=CC(OC)=CC(OC)=C5)=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Lan JX, et al. Design, synthesis, bio-evaluation, and mechanism of action of novel allosecurinine derivatives as STAT3-based antitumor agents in vitro and in vivo. Bioorganic chemistry. 2026 Jun 15;180:110107. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
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AH-26

Alle STAT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

AH-26 Related Classifications

HY-184731 Related Classifications