ZAK-IN-2
ZAK-IN-2 (Compound 8) is a selective, covalent ZAK inhibitor with an IC50 of 11.5 nM. ZAK-IN-2 forms a covalent bond with Cys22 in the P-loop of ZAK to inhibit its kinase activity. ZAK-IN-2 inhibits the phosphorylation of the downstream target p38. ZAK-IN-2 blocks Doxorubicin (HY-15142A)-induced cleavage of Caspase 3. ZAK-IN-2 is applicable to research related to myocardial hypertrophy.
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- CAS No.: 3033697-19-4
- Formule: C33H26F2N8O4S
- Masse moléculaire:668.67
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
p38 |
Caspase 3 |
In Vitro
ZAK-IN-2 (60 min) potently inhibits recombinant ZAK kinase with an IC50 of 11.5 nM, and exhibits high selectivity over B-rafV600E[1].
ZAK-IN-2 (0.01-10 μM; 1 h) dose-dependently inhibits ZAKα kinase activity in U2OS cells, which is verified by the reduced phosphorylation level of downstream p38[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human U2OS osteosarcoma cells, CRISPR-generated ZAK knockout U2OS cells
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Concentration:10 μM
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Incubation Time:Undefined
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Result:Prevented doxorubicin-induced caspase 3 cleavage in U2OS cells, matching the effect seen in ZAK knockout cells.
Inhibited doxorubicin-induced phosphorylation of p38 and JNK.
Prevented massive cell death induced by 24 h doxorubicin treatment in U2OS cells, matching the protection seen in ZAK knockout cells.
Chemical Information
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CAS No. 3033697-19-4
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Masse moléculaire 668.67
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Formule C33H26F2N8O4S
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SMILES
O=C(N1CCC(C1)OC2=NNC3=C2C=C(C4=CN(C5=C(F)C(NS(=O)(C6=CC=CC(C7=CC=CC=C7)=C6)=O)=CC=C5F)N=N4)C=N3)C=C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ZAK-IN-2 Related Classifications
HY-182103 Related Classifications
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