β-carboline-ACS81
β-carboline-ACS81 is a β-carboline derivative with potent antitumor properties. β-carboline-ACS81 induces apoptosis through the collapse of mitochondrial membrane potential and arrests cell cycle at G2/M phase in HL-60 cells. β-carboline-ACS81 possesses potent antiproliferative activity against HL-60 cells (IC50 = 1.52 μM). β-carboline-ACS81 can be used for the research of leukemia, histiocytic lymphoma, hepatocellular carcinoma, malignant melanoma, colorectal carcinoma and lung carcinoma.
For research use only. We do not sell to patients.
- Formula: C26H27N3O2S2
- Molecular Weight:477.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
β-carboline-ACS81 (Compound 12c) (72 h) exhibits significant anti-proliferative activity against tumor cell lines, with IC50 values of 1.52, 2.03, 2.8, 6.04, and 6.57, 37.23 μM for HL-60, U937, HepG2, HCT-116, A375 and A549 respectively, compared with an IC50 value of 33.92 μM in normal L-02 cells[1].
β-carboline-ACS81 (0.38-1.52 μM, 48 h) induces G2/M phase arrest, thereby inhibiting cell proliferation, and apoptosis in HL-60 cells, with the latter potentially mediated by mitochondrial pathway involvement as evidenced by diminished mitochondrial membrane potential[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60 cells
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Concentration:0.38, 0.76 and 1.52 μM
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Incubation Time:48 h
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Result:Induced a gradual increase in the proportion of cells in the G2/M phase with the rising concentrations.
Elevated G2/M phase cell percentage from 18.75% in the blank control group to 20.58%, 25.63%, and ultimately to 31.28%.
Caused a continuous decrease in the number of cells in the G1 phase, which dropped from 65.97% in the blank control group to 61.82%, 58.39%, and 50.82%, respectively.
Induced little effect on the number of cells in the S phase, which remained largely unchanged.
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Cell Line:HL-60 cells
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Concentration:0.38, 0.76 and 1.52 μM
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Incubation Time:48 h
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Result:Induced progressive chromatin condensation and cell membrane disruption in correlation with the concentration.
Preserved normal nuclear morphology in most cells but induced increased fluorescence (early chromatin condensation) in some cells at 0.38 μM.
Induced intense nuclear fluorescence (pyknosis) in numerous cells and clear nuclear fragmentation into variable bright blue particles (apoptotic bodies) at 0.76 μM.
Eliminated normal nuclear morphology, with most cells showing advanced nuclear pyknosis and karyorrhexis that formed dense, intensely fluorescent blue granular aggregates at 1.52 μM.
Caused a dose-dependent increase in apoptotic cells to 14.73%, 27.68%, and 40.89% at escalating concentrations.
Chemical Information
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Molecular Weight 477.64
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Formula C26H27N3O2S2
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SMILES
CN(C)C1=CC=C(C2=NC(COC(CCSSCC=C)=O)=CC3=C2NC4=C3C=CC=C4)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)