RIP2 Kinase Inhibitor 4
Names
[ CAS No. ]:
2126803-41-4
[ Name ]:
RIP2 Kinase Inhibitor 4
Biological Activity
[Description]:
RIP2 Kinase Inhibitor 4 is a potent and selective RIPK2 PROTAC. RIP2 Kinase Inhibitor 4 effectively degrades RIPK2 (pIC50 of 8) and inhibits the release of related TNF-α[1].
[Related Catalog]:
[Target]
cIAP1
RIPK2:8 (pIC50)
[In Vitro]
RIP2 Kinase Inhibitor 4 (Compound 20) utilizes a novel inhibitor of apoptosis (IAP) binder. RIP2 Kinase Inhibitor 4 possess comparatively reduced binding potency at both cIAP1 and XIAP BIR3 domains and increased potency at the XIAP BIR2 domain[1]. RIP2 Kinase Inhibitor 4 (Compound 20) recruits the IAP E3 ligases and shows markedly reduced inhibition of muramyl dipeptide (MDP)-stimulated TNFα production in human peripheral blood mononuclear cells (PBMCs) (pIC50 of 9.3)[1].
[In Vivo]
The initial in vivo assessment of RIP2 Kinase Inhibitor 4 (Compound 20) in rats dosed at 0.5 mg/kg SC demonstrated high levels of RIPK2 degradation and inhibition of MDP-stimulated TNFα release at the final 48 h time point[1].
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C50H66F2N14O7S
[ Molecular Weight ]:
1045.21