QS-57
QS-57 is a heterobifunctional targeted protein localization (TPL) agent. QS-57 binds to BRD4 via its JQ1 domain and covalently targets 14-3-3σ to form a ternary complex. QS-57 sequesters nuclear BRD4 in the cytoplasm, impairing the nuclear transcriptional regulatory function mediated by BRD4. QS-57 significantly reduces the nuclear BRD4 protein level and increases the cytoplasmic BRD4 protein abundance in cancer cells. QS-57 can be used for research on breast cancer and colorectal cancer.
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- Fòrmula: C39H43ClN8O3S
- Peso molecular:739.33
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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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BRD4 |
14-3-3σ |
QS-57 (25 μM; 24 h) sequesters nuclear BRD4 into the cytoplasm in T47D breast cancer cells, significantly reducing nuclear BRD4 levels and increasing cytoplasmic BRD4 levels[1].
QS-57 (100 μM; 3-24 h) sequesters nuclear BRD4 into the cytoplasm in HCT116 colorectal cancer cells, while pre-treatment with JQ1 (HY-13030) significantly attenuates this effect. This effect also completely abrogates in 14-3-3σ-knockout HCT116 cells[1].
QS-57 (100 μM; 24 h) induces the formation of a ternary complex between wild-type 14-3-3σ and BRD4 in HEK293 cells, while this effect is abolished in cells expressing the 14-3-3σC38S/C96S mutant[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T47D breast cancer cells
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Concentration:25 μM
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Incubation Time:24 h
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Result:Significantly reduced nuclear BRD4 protein levels relative to vehicle-treated controls.
Substantially increased cytosolic BRD4 levels relative to vehicle-treated controls.
Left nuclear loading control histone levels unchanged.
Left cytosolic loading control GAPDH levels unchanged.
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Cell Line:HCT116 colorectal cancer cells
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Concentration:100 μM (QS-57); 100 μM (JQ1 pretreatment)
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Incubation Time:24 h (QS-57)
6 h (JQ1 pretreatment) -
Result:Significantly increased cytosolic BRD4 levels relative to vehicle-treated controls.
Had its cytosolic BRD4 accumulation effect significantly attenuated by pretreatment with 100 μM JQ1 for 6 h.
JQ1 treatment alone did not result in cytosolic BRD4 accumulation.
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Cell Line:Wild-type and 14-3-3σ knockout HCT116 colorectal cancer cells
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Concentration:100 μM
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Incubation Time:24 h
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Result:Significantly increased cytosolic BRD4 levels in wild-type HCT116 cells.
Completely attenuated the cytosolic BRD4 increase effect in 14-3-3σ knockout HCT116 cells.
Left cytosolic loading control GAPDH levels unchanged across all groups.
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Cell Line:Wild-type and 14-3-3σ knockout HCT116 colorectal cancer cells
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Concentration:100 μM
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Incubation Time:3 h
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Result:Induced clearly visible cytosolic BRD4 accumulation in wild-type HCT116 cells.
Showed no detectable cytosolic BRD4 accumulation in vehicle-treated wild-type HCT116 cells.
Did not induce cytosolic BRD4 sequestration in QS-57-treated 14-3-3σ knockout cells.
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Cell Line:HEK293 cells expressing FLAG-tagged wild-type or C38S/C96S mutant 14-3-3σ
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Concentration:100 μM
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Incubation Time:24 h
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Result:Induced ternary complex formation between wild-type 14-3-3σ and BRD4, shown by enriched BRD4 in FLAG pulldowns.
Abrogated ternary complex formation in cells expressing the C38S/C96S mutant 14-3-3σ.
Did not enrich negative control GAPDH in FLAG pulldowns.
Chemical Information
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Peso molecular 739.33
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Fòrmula C39H43ClN8O3S
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SMILES
C=CC(N1CCC2(C1)CCN(C2)CC3=CC=C(C=C3)C(NCCNC(C[C@@H]4N=C(C5=C(N6C(C)=NN=C46)SC(C)=C5C)C7=CC=C(C=C7)Cl)=O)=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)
QS-57 Related Classifications
HY-169081 Related Classifications
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