Name | HS1371 |
Synonyms | HS1371 HS1371 HS-1371 CS-2831 HS 1371 2158197-70-5 Quinoline, 4-(4-methylphenoxy)-7-[1-(4-piperidinyl)-1H-pyrazol-4-yl]- |
CAS | 2158197-70-5 |
Molecular Formula | C24H24N4O |
Molar Mass | 384.47 |
Solubility | DMSO : 16.67 mg/mL (43.36 mM; Need ultrasonic) |
Storage Condition | Keep in dark place,Inert atmosphere,Room temperature |
Use | HS-1371 is a novel kinase inhibitor of RIP3-mediated necroptosis. HS-1371 directly binds to RIP3 in an ATP-competitive and time-independent manner, providing a mechanism of action. Moreover, the compound inhibited TNF-induced necroptosis but did not inhibit TNF-induced apoptosis, indicating that this novel inhibitor has a specific inhibitory effect on RIP3-mediated necroptosis via the suppression of RIP3 kinase activity. HS-1371 could serve as a potential preventive or therapeutic agent for diseases involving RIP3 hyperactivation. |
In vitro study | HS-1371 has an inhibitory effect on the phosphorylation of RIP3 in the S227 site. In HT-29 cells, it had complete inhibitory activity on TNF-induced necroptosis signals and no activity on phosphorylation of RIP3 and MLKL. The formation of the necrosis complex can be prevented by HS-1371 inhibition of RIP3 kinase activity, disrupting the recruitment of MLKL. TNF-induced cell necrosis was rescued by HS-1371. It protects cells from rip3-dependent necrotic cell death, but does not affect apoptotic cell death. |
Reference Show more | 1. Park HH, et al. HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis. Exp Mol Med. 2018 Sep 20;50(9):125 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.601 ml | 13.005 ml | 26.01 ml |
5 mM | 0.52 ml | 2.601 ml | 5.202 ml |
10 mM | 0.26 ml | 1.3 ml | 2.601 ml |
5 mM | 0.052 ml | 0.26 ml | 0.52 ml |