5.32757

RIPK2 Inhibitor, OD36

• Synonym(s): RIPK2 Inhibitor, OD36, RIPK2 inhibitor, RIP kinase inhibitor
• Empirical Formula (Hill Notation): C₁₆H₁₅ClN₄O₂
• CAS Number: 1638644-62-8
• Molecular Weight: 330.77
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥97% (HPLC)
• Quality Level: 100
• form: powder
• potency: 5.3 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: light beige
• solubility: DMSO: 50 mg/mL
• storage temp.: −20°C

Description

General description

A cell permeable, highly potent, selective, and ATP-competitive inhibitor of receptor-interacting protein 2 (RIPK2, IC₅₀ = 5.3 nM).

A cell permeable, pyrazolopyridine containing macrocycle derivative that acts as a highly potent, selective, ATP-competitive and reversible inhibitor of receptor-interacting protein 2 (RIPK2, IC₅₀ = 5.3 nM). Shown to minimally affect the activity of 366 other protein kinases. At higher concentrations (100 nM), inhibits ALK-2, salt-inducible kinase 2 (SIK2), activin receptor type-2B (ACVR2B), and activin A receptor type II-like 1 (ACVRL1) by ~80%. Blocks RIPK2 autophosphorylation and downstream NF-κB and MAP kinase signaling induced by muramyl dipeptide (MDP), and reduces MDP-induced cellular infiltration of neutrophils and lymphocytes in an in vivo peritonitis model (6.25 mg/kg, i.p.).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

A cell permeable, pyrazolopyrinide containing macrocycle derivative that acts as a highly potent, selective, and ATP-competitive inhibitor of receptor-interacting protein 2 (RIPK2, IC₅₀ = 5.3 nM). At ~20-fold higher concentration inhibits (~80% inhibition at 100 nM) the activity of ALK-2, salt-inducible kinase 2 (SIK2), activin receptor type-2B (ACVR2B), and activin A receptor type II-like 1(ACVRL1), but does not affect the activity of 366 other protein kinases. Blocks RIPK2 autophosphorylation and downstream NF-κB and MAP kinase signaling induced by muramyl dipeptide (MDP) and reduces MDP-induced cellular infiltration of neutrophils and lymphocytes in an in vivo peritonitis model (6.25 mg/kg).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
RIPK2

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Tigno-Aranjuez, J.T., et al. 2014. J. Biol. Chem.289, 29651.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable