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2126803-41-4

2126803-41-4 structure
2126803-41-4 structure
  • Name: RIP2 Kinase Inhibitor 4
  • Chemical Name: RIP2 Kinase Inhibitor 4
  • CAS Number: 2126803-41-4
  • Molecular Formula: C50H66F2N14O7S
  • Molecular Weight: 1045.21
  • Catalog: Signaling Pathways Apoptosis RIP kinase
  • Create Date: 2021-12-23 12:08:33
  • Modify Date: 2024-01-11 13:43:47
  • 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].

Name RIP2 Kinase Inhibitor 4
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

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

Molecular Formula C50H66F2N14O7S
Molecular Weight 1045.21