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Referencia número: HY-183786

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Anticancer agent 327

Anticancer agent 327, a fluorescent Andrographolide (HY-N0191) derivative, is an NF-κB p50 inhibitor. Anticancer agent 327 covalently binds to the p50 subunit of NF-κB. Anticancer agent 327 reduces levels of multiple oncogenic p53 proteins via the autophagy/lysosome pathway. Anticancer agent 327 can be used for the research of pancreatic ductal adenocarcinoma (Ex/Em = 488/515 nm)^[1].

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₂₉H₃₆N₄O₈
Peso molecular:568.62

Almacenamiento:

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

Anticancer agent 327 Chemical Structure

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Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas NF-κB :

In Vitro

Anticancer agent 327 (Compound 4) (1-30 μM; 48 h) potently reduces viability of PANC-1 and MIA PaCa-2 PDAC cells with IC₅₀ values of 9.94 μM and 25.30 μM, respectively^[1].
Anticancer agent 327 (1-30 μM; 2-24 h) significantly reduces levels of oncogenic p53^R273H in PANC-1 cells and p53^R248W in MIA PaCa-2 cells in a concentration- and time-dependent manner^[1].
Anticancer agent 327 (10 μM; 24 h) reduces oncogenic p53^R273H protein levels in PANC-1 cells primarily through the autophagy pathway^[1].
Anticancer agent 327 (1-30 μM; 24 h) potently inhibits long-term proliferation of PANC-1, MIA PaCa-2, and KPC PDAC cells, with the greatest activity against PANC-1 cells^[1].
Anticancer agent 327 (1-30 μM; 10-24 h) suppresses migration of PANC-1, MIA PaCa-2, and KPC PDAC cells in a concentration-dependent manner, with the strongest activity against KPC cells^[1].
Anticancer agent 327 (5-10 μM; 12 h) downregulates transcription of multiple cancer-related genes downstream of oncogenic TP53^R273H, without altering TP53 mRNA levels^[1].
Anticancer agent 327 (6 μM; 5 min-48 h) is rapidly taken up by PANC-1 cells, with detectable fluorescent signals within 5 min, and remains stably retained for at least 48 h^[1].
Anticancer agent 327 (1-10 μM; 1 h at 25 °C) covalently binds to the NF-κB p50 subunit in vitro in a concentration-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay^[1]

Cell Line:

human pancreatic ductal adenocarcinoma (PDAC) cell lines PANC-1 (p53^R273H), MIA PaCa-2 (p53^R248W)
Concentration:

1 μM; 3 μM; 10 μM; 30 μM
Incubation Time:

48 h
Result:

Exhibited concentration-dependent cytotoxicity in both cell lines.
Had an IC₅₀ of 9.94 μM in PANC-1 cells, with significant viability reduction at all tested concentrations.
Had an IC₅₀ of 25.30 μM in MIA PaCa-2 cells, with significant viability reduction at 30 μM.

Western Blot Analysis^[1]

Cell Line:

human PDAC PANC-1 (p53^R273H) cells
Concentration:

1 μM; 3 μM; 5 μM; 10 μM; 20 μM
Incubation Time:

2 h; 6 h; 12 h; 24 h
Result:

Significantly upregulated the autophagy marker LC3-II.
Caused time-dependent and concentration-dependent reduction of p53^R273H.

Western Blot Analysis^[1]

Cell Line:

MIA PaCa-2 (p53^R248W)
Concentration:

3 μM; 5 μM; 10 μM; 20 μM; 30 μM
Incubation Time:

2 h; 6 h; 12 h; 24 h
Result:

Caused time-dependent and concentration-dependent reduction of p53^R248W levels.

Cell Proliferation Assay^[1]

Cell Line:

human PDAC cell lines PANC-1 (p53^R273H), MIA PaCa-2 (p53^R248W), mouse PDAC cell line KPC (p53^R172H)
Concentration:

1 μM; 3 μM; 5 μM; 10 μM; 30 μM
Incubation Time:

24 h
Result:

Significantly suppressed colony formation in all three cell lines in a concentration-dependent manner.
Showed the strongest effect on colony formation in PANC-1 cells.

Cell Migration Assay ^[1]

Cell Line:

human PDAC cell lines PANC-1 (p53^R273H), MIA PaCa-2 (p53^R248W), mouse PDAC cell line KPC (p53^R172H)
Concentration:

1 μM; 3 μM; 10 μM; 30 μM
Incubation Time:

10 h; 12 h; 24 h
Result:

Suppressed migration of PANC-1 and KPC cells in a concentration-dependent manner, with no apparent cytotoxicity during the incubation period.
Reduced migration of MIA PaCa-2 cells only at 30 μM, with cytotoxicity observed at this concentration.
Caused greater suppression of migration in KPC cells than PANC-1 cells.

Real Time qPCR^[1]

Cell Line:

human PDAC PANC-1 (p53^R273H) cells
Concentration:

5 μM; 10 μM
Incubation Time:

12 h
Result:

Significantly reduced mRNA levels of CCNA2, PCNA, CXCL1, CXCL2, CXCL8, TIGAR, and MYC in a concentration-dependent manner.
Did not affect TP53 mRNA levels, indicating post-transcriptional regulation of p53^R273H.
Suppressed MYC expression, unlike andrographolide.

In Vivo

Anticancer agent 327 (Compound 4) (10-20 mg/kg; i.p.; every 2 days; 4 total doses) exhibits no observable in vivo toxicity in 4-week-old immunocompetent C57BL/6 mice at the tested dosing regimen^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6 (male; 4 weeks old)^[1]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

i.p.; every 2 days; 4 total doses
Result:

Did not affect the body weights of treated mice.
Showed no evident liver or kidney toxicity, as indicated by serum biochemical parameters and histological analyses of liver and kidney tissues.

Chemical Information

Peso molecular 568.62
Fòrmula C₂₉H₃₆N₄O₈
SMILES

CN(CC1OC[C@]([C@](CCC([C@H]2C/C=C3C(OC[C@H]/3O)=O)=C)([H])[C@@]2(C)CC4)(C)[C@@H]4O1)C5=CC=C([N+]([O-])=O)C6=NON=C56
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]. Li YR, et al. Design, synthesis, and evaluation of novel andrographolide derivatives as anti-pancreatic cancer therapeutics. Bioorg Chem. 2026;178:109946. [Content Brief]

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Anticancer agent 327

Ver todos los productos específicos de isoformas NF-κB

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Anticancer agent 327 Related Classifications

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