HsClpP activator-2
HsClpP activator-2 is an orally active HsClpP agonist with a KD of 40 nM. HsClpP activator-2 potently inhibits SCLC cells including H69 (IC50 = 0.17 μM) and H82 (IC50 = 0.19 μM). HsClpP activator-2 disrupts mitochondrial membrane potential (MMP), as well as induces apoptosis and ROS in H82 cells. HsClpP activator-2 significantly inhibits tumor growth in non-SMC xenograft models with a tumor growth inhibition. HsClpP activator-2 can be used for the study of small cell lung carcinoma (SCLC).
For research use only. We do not sell to patients.
- Formula: C29H26F3N3O2
- Molecular Weight:505.53
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HsClpP 40 nM (Kd) |
HsClpP activator-2 (Compound 8o) (0.02-10 μM, 72 h) shows potent antiproliferative activity against H69, H82, and non-SMC cells, with IC50 values of 0.17 μM, 0.19 μM, and 0.1 μM, respectively[1].
HsClpP activator-2 (100-400 nM, 72 h) induces dose-dependent degradation of mitochondrial OXPHOS complex proteins (NDUFB8, SDHB, UQCRC2, MTCO1, ATP5A) in H82 cells[1].
HsClpP activator-2 (100-400 nM, 72 h) significantly reduces intracellular ATP levels and increases ROS levels in H82 cells in a dose-dependent manner[1].
HsClpP activator-2 (100-400 nM, 48-72 h) disrupts mitochondrial membrane potential (MMP) and induces apoptosis in H82 cells[1].
HsClpP activator-2 (100-400 nM, 24-48 h) inhibits colony formation and migration of non-SMC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H82 cells
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Concentration:100, 200, 400 nM
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Incubation Time:72 h
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Result:Induced dose-dependent degradation of mitochondrial OXPHOS complex proteins (NDUFB8, SDHB, UQCRC2, MTCO1, ATP5A) in H82 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Non-SMC cells (1×106 cells) were subcutaneously implanted into the flanks of 6-8-week-old male BALB/c nude mice (18-22 g)[1]
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Dosage:1.3, 2.5, 5 mg/kg
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Administration:i.p., twice weekly, 20 days
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Result:Achieved tumor growth inhibition (TGI) rates of 37.03%, 49.12%, and 60.44% for tumor weight, as well as 41.93%, 50.08%, and 63.01% for tumor volume at doses of 1.3, 2.5, and 5 mg/kg, respectively.
Showed no significant changes in body weight and no pathological damage in major organs (heart, liver, spleen, lung, kidney).
Reduced the Ki67 expression.
Increased the Caspase 3 expression in tumor.
Chemical Information
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Molecular Weight 505.53
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Formula C29H26F3N3O2
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SMILES
O=C(C1=C(C2=CC=C(CO)C=C2)CCN(CC3=CC=CC(C#N)=C3)C1)NCC4=CC=C(C(F)(F)F)C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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