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RIP2 Kinase Inhibitor 4

Catalog No. T39574 CAS 2126803-41-4

RIP2 Kinase Inhibitor 4 is a highly potent and selective RIPK2 PROTAC compound that efficiently degrades RIPK2 (with a pIC50 value of 8) and effectively inhibits the release of TNF-α.

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RIP2 Kinase Inhibitor 4 Chemical Structure

RIP2 Kinase Inhibitor 4, CAS 2126803-41-4

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Biological Description

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Description	RIP2 Kinase Inhibitor 4 is a highly potent and selective RIPK2 PROTAC compound that efficiently degrades RIPK2 (with a pIC50 value of 8) and effectively inhibits the release of TNF-α.
In vitro	RIP2 Kinase Inhibitor 4 (Compound 20) is a novel inhibitor that targets the apoptosis (IAP) binder, displaying lower binding efficiency to the cIAP1 and XIAP BIR3 domains while showing enhanced binding to the XIAP BIR2 domain[1]. Moreover, this compound demonstrates the ability to recruit IAP E3 ligases, significantly diminishing its suppression of muramyl dipeptide (MDP)-induced TNFα production in human peripheral blood mononuclear cells (PBMCs), indicated by a pIC50 value of 9.3[1].
In vivo	The initial in vivo evaluation of RIP2 Kinase Inhibitor 4 (Compound 20) in rats, administered subcutaneously at a dose of 0.5 mg/kg, showed significant degradation of RIPK2 and suppression of MDP-induced TNFα release after 48 hours[1].

Molecular Weight	1045.23
Formula	C50H66F2N14O7S
CAS No.	2126803-41-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

RIP2 Kinase Inhibitor 4 2126803-41-4 RIP-2 Kinase Inhibitor 4 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.