MW01
MW01 is a CLK2/CLK4 inhibitor with IC50 values of 360 nM and 14.1 nM, respectively. MW01 blocks DNA damage-induced IKK/NF-κB signaling and reduces p65 nuclear translocation/phosphorylation as well as radiation-induced IKK-γ phosphorylation/monoubiquitination. MW01 weakly activates γ-H2AX without increasing cleaved caspase-3, and enhances apoptosis by perturbing the NF-κB/p53 axis. MW01 can be used for research on cancer and glioblastoma.
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- No. CAS: 904504-22-9
- Fòrmula: C20H14N2O4
- Peso molecular:346.34
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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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Actividad biológica
Descripciòn
IC50 & Target
[1]|
CLK2 360 nM (IC50) |
CLK4 14.1 nM (IC50) |
IKK |
NF-κB |
p65 |
IKK-γ |
γ-H2AX |
p53 |
In Vitro
MW01 (10 µM; 1 h pre-exposure) abolishes IR-induced BIRC3 mRNA upregulation in U2-OS cells[1].
MW01 (10 µM; 6-48 h) alone is minimally toxic but sensitizes U2-OS cells to Etoposide-induced viability loss[1].
MW01 is cell-permeable in CaCo2 monolayers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U2-OS and HEK293
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Concentration:10 µM
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Incubation Time:1 h (MW01 pre-exposure); 20 min (TNFα); 90 min; 45 min; 8 h; 24 h
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Result:Reduced p65 S536 phosphorylation only after DNA damage, leaving TNFα-stimulated and unstimulated levels unchanged; caused complete reduction of p-Akt.
Inhibited IR-induced IKKγ S85 phosphorylation and K285 monoubiquitination but did not inhibit PARP1 activation/PAR formation or nuclear ATM activation.
Potentiated PARP1 cleavage.
Caused weak γH2AX activation and p53 stabilization without increasing cleaved caspase-3; Etoposide co-exposure increased cleaved caspase-3 with persistent γH2AX.
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Cell Line:U2-OS
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Concentration:10 µM
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Incubation Time:1 h (MW01 pre-exposure); 8 h
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Result:Abolished IR-induced upregulation of BIRC3 mRNA.
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Cell Line:U2-OS
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Concentration:10 µM
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Incubation Time:6 h; 24 h; 48 h
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Result:Slightly reduced cell viability at 6, 24, and 48 h compared with DMSO-treated controls, without gross cell death at 48 h.
Co-exposure with Etoposide significantly reduced cell viability after 6 h compared with Etoposide alone; at 24 h, attached cells were visibly distressed and floating cells increased, with a greater effect at 48 h.
The same viability reduction was confirmed with cisplatin co-exposure.
- Kinase activity and phosphorylation assays
- Cytoplasmic-Nuclear Fractionated Protein Extraction
- Western Blot
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- Research Protocol for Inflammation-related Diseases
- Protocol for Kinase activity and phosphorylation assays
- Genotoxicity/Mutagenicity Study
Chemical Information
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No. CAS 904504-22-9
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Peso molecular 346.34
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Fòrmula C20H14N2O4
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SMILES
O=C1C2=C(C3=NC=CC4=C3N1C5=C4C=C(C=C5)O)C=CC(OC)=C2OC
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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)
MW01 Related Classifications
HY-187968 Related Classifications
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