Anticancer agent 324
Anticancer agent 324 is a Survivin inhibitor. Anticancer agent 324 competitively binds to Survivin’s linker region and triggers proteasomal IAP degradation. Anticancer agent 324 blocks Borealin binding and chromosomal passenger complex formation, and inhibits Survivin-CRM1 nuclear-cytoplasmic transport. Anticancer agent 324 activates extrinsic (caspase-8) and intrinsic (caspase-9) apoptotic pathways, activates executioner caspases-3 and caspases-7, and arrests cell cycle. Anticancer agent 324 can be used for the research of breast cancer.
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- 화학식: C85H130N28O21S
- 분자량:1912.18
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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Caspase-3 |
Caspase-7 |
Caspase-8 |
Caspase-9 |
Anticancer agent 324 (Compound P3) binds with higher affinity to the linker region of Survivin than cIAP1, NAIP, and XIAP, enabling it to competitively disrupt Survivin's protective interactions with these IAP family members[1].
Anticancer agent 324 (5-50 μM; 24-48 h) reduces MCF-7 human breast cancer cell viability in a time-dependent manner[1].
Anticancer agent 324 (15-45 μM; 24-48 h) induces caspase-3 and -7 activity in MCF-7 human breast cancer cells in vitro in a time-dependent manner[1].
Anticancer agent 324 (25 μM; 48 h) significantly activates both caspase-8 (extrinsic pathway) and caspase-9 (intrinsic pathway) in MCF-7 human breast cancer cells[1].
Anticancer agent 324 (25 μM; 48 h) significantly increases apoptosis and mitotic catastrophe in MCF-7 human breast cancer cells after 48 h incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:5 μM; 10 μM; 15 μM; 20 μM; 25 μM; 30 μM; 35 μM; 40 μM; 45 μM; 50 μM
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Incubation Time:24 h; 48 h
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Result:Reduced MCF-7 cell viability in a time-dependent manner.
Reached an IC50 of 40 μM at 24 h and 25 μM at 48 h.
Showed significant reductions in viability at all tested concentrations relative to control at 48 h, with effect sizes (Cohen's d) ranging from 6.20 to 19.52.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:15 μM; 25 μM; 35 μM; 45 μM
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Incubation Time:24 h; 48 h
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Result:Increased total apoptosis to 82.78% at 25 μM, with significant increases in early apoptosis (18.7%, p = 0.0044, Cohen's d = -4.73) and late apoptosis (64.1%, p = 2.86e-05, Cohen's d = -17.4), and minimal non-significant necrosis (1.36%, p = 0.0868).
Increased total apoptosis to 23.23% at 45 μM, with significant increases only in late apoptosis (19.2%, p = 0.001, Cohen's d = 5.53) and necrosis (13.1%, p = 0.0043, Cohen's d = 5.86), while early apoptosis did not change significantly (p = 0.462).
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Cell Line:MCF-7 human breast cancer cells
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Concentration:25 μM
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Incubation Time:48 h
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Result:Significantly increased the proportion of non-viable cells (red fluorescence from PI) relative to control (p = 0.00011), confirming induction of apoptosis and mitotic catastrophe.
Chemical Information
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분자량 1912.18
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화학식 C85H130N28O21S
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Sequence
Arg-Arg-Arg-Leu-Arg-Glu-Met-Asn-Trp-Val-Asp-Tyr-Phe-Ala
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Sequence Shortening
RRRLREMNWVDYFA
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Anticancer agent 324 Related Classifications
HY-P11828 Related Classifications
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