1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis Epigenetics
  2. ClpP Mitochondrial Metabolism Apoptosis Caspase PARP
  3. 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.

For research use only. We do not sell to patients.

MS6076

MS6076 Chemical Structure

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Description

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[1].

IC50 & Target[1]

Caspase 3

 

In Vitro

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.

Western Blot Analysis[1]

Cell Line: MDA-MB-468
Concentration: 25, 50, 100, 150, 200 nM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: MDA-MB-468
Concentration: 1.0 μM
Incubation Time: 72 h
Result: Reduced full-length caspase 3 and PARP protein levels.
Increased levels of cleaved caspase 3 and cleaved PARP, similar to positive control doxorubicin.
In Vivo

MS6076 (50 mg/kg; i.p.; single dose) is bioavailable and well tolerated in male Swiss Albino mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Swiss Albino (male)[1]
Dosage: 50 mg/kg
Administration: i.p.; single dose
Result: Maintained high plasma concentrations with 8 h.
Molecular Weight

524.54

Formula

C27H27F3N6O2

SMILES

O=C1N(C2=NCCN2C3=C1CN(CC4=CC(C#N)=CC=C4)CC3)CC5=CC=C(C=C5OCCN)C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MS6076
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HY-178749
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