XSJ151
XSJ151 is a topoisomerase I inhibitor, stabilizing the DNA-Topo I covalent complex and inducing DNA double-strand breaks. XSJ151-induces DNA damage activates the p53-p21 signaling pathway, specifically regulating the expression of cyclins, leading to G2/M phase cell cycle arrest and disrupting the dynamic homeostasis of Bcl-2 family proteins, thereby triggering apoptosis in gastric cancer cells. XSJ151 can be used for the study of gastric cancer.
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- No. CAS: 1685279-23-5
- Fòrmula: C37H31N5O10S
- Peso molecular:737.73
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
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Topoisomerase I |
Bcl-2 |
Bax |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.0149 μM
Compound: 13j
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Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B colorimetric assay
Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B colorimetric assay
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[PMID: 26994847] |
XSJ151 (48 h) exhibits strong cytotoxicity against gastric cancer cell lines, including AGS (IC50 = 0.088 μM), MGC803 (IC50 = 0.592 μM), HGC27 (IC50 = 1.951 μM), and SGC7901 (IC50 = 11.121 μM), while showing lower cytotoxicity against normal cell lines such as GES-1 (IC50 = 0.202 μM) and HIEC (IC50 > 40 μM)[1].
XSJ151 (0.1-2.5 nM, 7-10 days) inhibits gastric cancer cell colony formation in a concentration-dependent manner. In AGS cells, 2.5 nM XSJ151 reduces the colony count from 74 to 22; in MGC803 cells, it reduces it from 68 to 21[1].
XSJ151 (2.5-10 nM, 24 h) dose-dependently induces G2/M phase arrest in AGS and MGC803 gastric cancer cells, leading to significant enrichment of the G2/M-phase population[1].
XSJ151 (44-600 nM, 48 h) significantly upregulates the expression of G2/M phase-related proteins (p53, p21, CCNB) and the S phase marker CCNA in AGS and MGC803 cells, while the G1 phase-specific protein CCNE is downregulated in a dose-dependent manner[1].
XSJ151 (88–600 nM, 48 h) induces apoptosis in AGS and MGC803 cells by significantly upregulating BAD and BAX proteins and downregulating Bcl-2 protein[1].
XSJ151 (88-600 nM, 48 h) significantly increases the number of γ-H2AX intranuclear spots in AGS and MGC803 cells, indicating DNA double-strand breaks and significantly increased γ-H2AX protein levels[1].
XSJ151 (150-200 μM, 30 min) effectively inhibits Topo I-catalyzed DNA relaxation[1].
XSJ151 (44-600 μM, 48 h) significantly downregulates Topo I protein in AGS and MGC803 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AGS cells, MGC803 cells
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Concentration:2.5 nM, 5 nM, 10 nM
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Incubation Time:24 h
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Result:In AGS cells, the proportion of cells in G2/M phase increased from 14.96% to 65.45%.
In MGC803 cells, increased from 16.74% to 71.65%.
Chemical Information
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No. CAS 1685279-23-5
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Peso molecular 737.73
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Fòrmula C37H31N5O10S
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SMILES
COC(C=C1)=CC=C1CC(NCC(O[C@]2(CC)C(OCC3=C2C=C4N(CC5=CC6=CC=CC=C6N=C54)C3=O)=O)=O)=NS(C7=CC=C([N+]([O-])=O)C=C7)(=O)=O
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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)
XSJ151 Related Classifications
HY-179520 Related Classifications
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