Sigma-Aldrich Ripk2 Inhibitor, Od36 - Ca

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

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 anin vivoperitonitis 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 anin vivoperitonitis model (6.25 mg/kg).

Biochem/Physiol Actions

Cell permeable: yesPrimary 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.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany