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HWY336 is a selective, non-ATP competitive dual MKK4 and MKK7 inhibitor with IC50 values of 6 µM on MKK4 and 10 µM on MKK7 in vitro. HWY336 inhibits the phosphorylation of MKK4/MKK7 inside the activation loop or hinders the substrate to access the kinase. HEK293T cells that were treated with D-sorbitol, to activate JNK, were incubated with HWY336 in increasing concentrations. The phosphorylation of JNKs was reduced after 3 h of incubation with 9 µM HWY336 and disappeared after 4 h of treatment with 12 µM HWY336. These experiments and the performed wash experiments indicate that the inhibition is directed to MKK4, is reversible and is non-covalent.
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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