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Cat. No.: HY-136010

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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.

For research use only. We do not sell to patients.

CAS No.: 2126803-41-4
Formula: C₅₀H₆₆F₂N₁₄O₇S
Molecular Weight:1045.21

Storage:

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

Data Sheet (268 KB)

RIP2 Kinase Inhibitor 4 Chemical Structure

CAS No.: 2126803-41-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

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].

IC₅₀ & Target^[1]

cIAP1

RIPK2

8 (pIC₅₀)

All RIP kinase Isoforms :

All PROTACs Isoforms :

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].

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

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].

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

Chemical Information

CAS No. 2126803-41-4
Molecular Weight 1045.21
Formula C₅₀H₆₆F₂N₁₄O₇S
SMILES

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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RIP2 Kinase Inhibitor 4

All RIP kinase Isoforms

All PROTACs Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

RIP2 Kinase Inhibitor 4 Related Classifications

HY-136010 Related Classifications