MS6076
MS6076 is a mitochondrial protease ClpP agonist. MS6076 specifically activates the ClpP protease in the mitochondrial matrix, significantly disrupting mitochondrial Electron Transport Chain (ETC) function by accelerating the degradation of unfolded proteins. MS6076 exhibits potent cytotoxicity against a variety of cancer cell lines. MS6076 induces cell apoptosis, increasing cleavage of caspase 3 and PARP. MS6076 can be used for the research of breast cancer.
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- Fòrmula: C27H27F3N6O2
- Peso molecular:524.54
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Caspase 3 |
MS6076 (0.313-10.0 μM; 15 min) stabilizes human ClpP in MDA-MB-468 cell lysates more potently than ONC212 (HY-111343), with effective stabilization observed at 0.313 μM[1].
MS6076 (1.0-10.0 μM; 2 min) binds and stabilizes purified human ClpP, as measured by a significant increase in thermal shift[1].
MS6076 (0.078-5.0 μM; 30 min) demonstrates potent cellular permeability and ClpP binding in live MDA-MB-468 cells[1].
MS6076 (25-200 nM; 24 h) activates ClpP-mediated proteolysis to degrade DAP13 in MDA-MB-468 cells[1].
MS6076 (50 nM; 12-48 h) disrupts mitochondrial respiration (basal, ATP-linked, and maximal) in MDA-MB-468 cells[1].
MS6076 (1.0 μM; 72 h) effectively induces apoptosis in MDA-MB-468 cells at 1.0 μM over 72 h, as evidenced by increased cleavage of caspase 3 and PARP[1].
MS6076 (72 h) potently reduces MDA-MB-468 breast cancer cell viability with an IC50 of 10.6 nM over 72 h[1].
MS6076 (72 h) potently reduces viability across multiple breast cancer cell lines, with IC50 values ranging from 7.0 to 13.9 nM[1].
MS6076 (72 h) potently reduces viability of ONC212-resistant MDA-MB-468 breast cancer cells with an IC50 of 27.7 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468
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Concentration:25, 50, 100, 150, 200 nM
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Incubation Time:24 h
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Result:Degraded more than 50% of DAP13 at 25 nM, while ONC212 did not significantly degrade DAP13 at this concentration.
Degraded DAP13 at 100, 150, and 200 nM, similar to ONC212.
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Cell Line:MDA-MB-468
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Concentration:1.0 μM
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Incubation Time:72 h
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Result:Reduced full-length caspase 3 and PARP protein levels.
Increased levels of cleaved caspase 3 and cleaved PARP, similar to positive control doxorubicin.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss Albino (male)[1]
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Dosage:50 mg/kg
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Administration:i.p.; single dose
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Result:Maintained high plasma concentrations with 8 h.
Chemical Information
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Peso molecular 524.54
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Fòrmula C27H27F3N6O2
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SMILES
O=C1N(C2=NCCN2C3=C1CN(CC4=CC(C#N)=CC=C4)CC3)CC5=CC=C(C=C5OCCN)C(F)(F)F
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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)
MS6076 Related Classifications
HY-178749 Related Classifications
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