Molecular Weight(MW): 384.47
HS-1371 is a potent RIP3 kinase inhibitor with an IC50 of 20.8 nM. It binds to the ATP binding pocket of RIP3 and inhibits ATP binding to prevent RIP3 enzymatic activity in vitro.
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|Description||HS-1371 is a potent RIP3 kinase inhibitor with an IC50 of 20.8 nM. It binds to the ATP binding pocket of RIP3 and inhibits ATP binding to prevent RIP3 enzymatic activity in vitro.|
HS-1371 shows an inhibitory effect on S227 auto-phosphorylation of RIP3 at the basal level. It displays a complete inhibitory effect on TNF-induced necroptosis signaling, showing no phosphorylation of RIP3 and MLKL in HT-29 cells. Inhibition of RIP3 kinase activity by HS-1371 blocks necrosome complex formation, showing disruption of MLKL recruitment. HS-1371 rescues cells from TNF-induced necroptosis. It rescues cells from RIP3-dependent necroptotic cell death but not apoptotic cell death.
Enzymatic assays:The inhibitory activities of all compounds toward RIP3 were measured by Reaction Biology Corp by means of radiometric kinase assays ([γ-32P]ATP). The enzymatic activity of RIP3 was monitored using 20 μM of myelin basic protein (MBP) dissolved in freshly prepared reaction buffer (20 mM HEPES (pH 7.5), 10 mM MgCl2, 1 mM EGTA, 0.02% BRIJ-35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, 1% DMSO). Each putative RIP3 inhibitor was dissolved in 100% DMSO at specific concentrations and serially diluted with epMotion 5070 in DMSO. Human RIP3 and 20 μM of peptide substrate (MBP) were added to the reaction buffer. After delivering the candidate inhibitor dissolved in DMSO to the kinase reaction mixture using Acoustic technology (Echo550; nanoliter range), the reaction mixture was incubated for 20 min at room temperature. To initiate the enzymatic reaction, 33P-ATP with specific activity of 10 μCi/μL was added to the reaction mixture to reach a final ATP concentration of 10 μM. Radioactivity was then monitored using the filter binding method after incubation of the reaction mixture for 2 h at room temperature. At given concentrations of inhibitor, biochemical potency was measured by the percent remaining kinase activity with respect to the vehicle (dimethyl sulfoxide) reaction. Curve fits and IC50 values were then obtained using the PRISM program. The ATP-competitive inhibitor staurosporine (STSP) was employed as a positive control in this study because of its high biochemical potency against various kinases including RIP3.
|In vitro||DMSO||13 mg/mL (33.81 mM)|
|Ethanol||4 mg/mL (10.4 mM)|
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