RIP2 Kinase Inhibitor 4 

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1045.21

C₅₀H₆₆F₂N₁₄O₇S

2126803-41-4

CC1=C(C)NN=C1NC2=NC=NC3=C2C=C(S(C(C)(C)C)(=O)=O)C(OCCCN4CCN(C5=NC=C(C(N[C@@H]6CN(C([C@H](C(C)(C)C)NC([C@H](C)NC)=O)=O)[C@H](C(NC(C(F)=CC=C7)=C7F)=O)C6)=O)N=C5)CC4)=C3

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Afjal H Miah, et al. Optimization of a Series of RIPK2 PROTACs. J Med Chem. 2021 Sep 9;64(17):12978-13003.  [Content Brief]