Title : Discovery of a Potent RIPK3 Inhibitor for the Amelioration of Necroptosis-Associated Inflammatory Injury.

Pub. Date : 2020

PMID : 33364238






4 Functional Relationships(s)
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1 Here, we discovered a small molecule Zharp-99 as a potent inhibitor of necroptosis through blocking the kinase activity of RIPK3. zharp-99 receptor-interacting serine-threonine kinase 3 Mus musculus
2 Zharp-99 strongly inhibits cellular activation of RIPK3, and MLKL upon necroptosis stimuli. zharp-99 receptor-interacting serine-threonine kinase 3 Mus musculus
3 Zharp-99 directly blocks the kinase activity of RIPK3 without affecting RIPK1 kinase activity at the tested concentration. zharp-99 receptor-interacting serine-threonine kinase 3 Mus musculus
4 Thus, our study demonstrates Zharp-99 as a potent inhibitor of RIPK3 kinase and also highlights its potential for further development of new approaches for treating necroptosis-associated inflammatory disorders. zharp-99 receptor-interacting serine-threonine kinase 3 Mus musculus