ClpP activator-2
ClpP activator-2 (Compound GU18) is a ClpP activator with a Kd of 5.01 μM for HsClpP. ClpP activator-2 enhances the proteolytic activity of HsClpP and promotes the degradation of α-casein by HsClpP, with an EC50 of 1.09 μM. ClpP activator-2 induces the accumulation of mitochondrial reactive oxygen species (ROS), leading to damage to mitochondrial structure and function. ClpP activator-2 exhibits significant in vivo anti-multiple myeloma activity.
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- No. CAS: 3036751-71-7
- Fòrmula: C22H19Cl2F3N4O
- Peso molecular:483.31
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Almacenamiento:
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
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| MV4-11 | IC50 |
10 μM
Compound: 7e
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Anti-leukemia activity against human MV4-11 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay
Anti-leukemia activity against human MV4-11 cells assessed as decrease in cell proliferation incubated for 72 hrs by CCK-8 assay
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[PMID: 38620134] |
ClpP activator-2 potently activates purified HsClpP with an EC50 of 0.54 ± 0.12 μM[1].
ClpP activator-2 (2 h) promotes the degradation of α-casein by HsClpP, with an EC50 of 1.09 ± 0.08 μM[1].
ClpP activator-2 binds to purified HsClpP, and its dissociation constant Kd is determined as 5.01 ± 1.05 μM by ITC[1].
ClpP activator-2 (0.45 μM; 24 h) causes significant mitochondrial ultrastructural damage to AMO.1 MM cells after treatment at 0.45 μM for 24 h[1].
ClpP activator-2 (0.15-0.6 μM; 48 h) promotes the accumulation of mitochondrial reactive oxygen species (ROS) in AMO.1 and ARP1 multiple myeloma (MM) cells in a concentration-dependent manner after 48 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human multiple myeloma cell lines AMO.1, ARP1
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Concentration:Gradient concentrations
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Incubation Time:24 h, 48 h, 72 h
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Result:Reduced cell viability in a time- and concentration-dependent manner.
For AMO.1 cells, reached IC50 values of 1.30 ± 0.08 μM (24 h), 0.68 ± 0.03 μM (48 h), and 0.08 ± 0.01 μM (72 h).
For ARP1 cells, reached IC50 values of 1.81 ± 0.14 μM (24 h), 0.86 ± 0.08 μM (48 h), and 0.21 ± 0.02 μM (72 h).
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Cell Line:Human multiple myeloma cell lines AMO.1, ARP1
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Concentration:0.15-0.6 μM
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Incubation Time:24 h
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Result:Induced dose-dependent G1 phase.
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Cell Line:Human multiple myeloma cell lines AMO.1, ARP1
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Concentration:0.15-0.6 μM (apoptosis assay); 0.45 μM (Western blotting)
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Incubation Time:24 h, 48 h, 72 h (apoptosis assay); 48 h (Western blotting)
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Result:Induced time- and concentration-dependent apoptosis, with 95% of AMO.1 cells and 73.8% of ARP1 cells apoptotic after 72 h of 0.6 μM treatment.
Upregulated cleaved caspase-3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID (female, 6-8 weeks old, subcutaneous xenograft model)[1]
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Dosage:5 mg/kg; 15 mg/kg; 30 mg/kg
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Administration:i.p.; every other day; 14 days
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Result:Achieved 56.7% tumor volume inhibition at 5 mg/kg.
Achieved 83.4% tumor volume inhibition at 15 mg/kg.
Achieved 91.4% tumor volume inhibition at 30 mg/kg.
Showed no treatment-related damage to major organs in the 30 mg/kg group compared to controls.
Chemical Information
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No. CAS 3036751-71-7
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Peso molecular 483.31
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Fòrmula C22H19Cl2F3N4O
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SMILES
O=C1NC(NCC2=CC=C(C(F)(F)F)C=C2)=NC3=C1CN(CC3)CC4=CC(Cl)=C(Cl)C=C4
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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)
ClpP activator-2 Related Classifications
HY-181934 Related Classifications
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- ClpP activator-2
- 3036751-71-7
- ClpP activator2
- ClpP activator 2
- ClpP
- Reactive Oxygen Species (ROS)
- Mitochondrial Metabolism
- caspase-3
- mitochondrial respiratory chain complexes I-V
- multiple myeloma
- AMO.1
- Homo sapiens caseinolytic protease P
- ARP1
- apoptosis
- NOD/SCID mice
- HsClpP
- mitochondrial dysfunction
- Inhibitor
- inhibitor
- inhibit