HS-1371 inhibits ATP binding to prevent RIP3 enzymatic activity. HS-1371 shows an inhibitory effect on S227 auto-phosphorylation of RIP3 at the basal level. 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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO: ≥ 12 mg/mL|
|Related RIPK Products|
|Necrostatin 2 racemate
Necrostatin-2 racemate (also known as 7-Cl-O-Nec-1 and Nec-1s) is a potent and specific receptor-interacting protein kinase 1 (RIPK1) inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.
GSK547 is a potent and highly selective receptor-interacting serine/threonine protein kinase 1 (RIPK1) inhibitor.
RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM.
GSK2982772 is a potent and selective RIP1 (Receptor Interacting Protein 1) kinase inhibitor, with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively.
|GSK2983559 free acid
GSK2983559 free acid is a potent, specific and oral bioavailable receptor interacting protein 2 (RIP2) kinase inhibitor.
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