产品
编 号：F749170
分子式：C50H66F2N14O7S
分子量：1045.21
分子式：C50H66F2N14O7S
分子量：1045.21
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CAS No: 2126803-41-4
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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.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).
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.
体内研究：
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.
体外研究：
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.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).
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