5.32757
RIPK2 Inhibitor, OD36
Synonim(y):
RIPK2 Inhibitor, OD36, RIPK2 inhibitor, RIP kinase inhibitor
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About This Item
Polecane produkty
Próba
≥97% (HPLC)
Poziom jakości
Postać
powder
siła działania
5.3 nM IC50
producent / nazwa handlowa
Calbiochem®
warunki przechowywania
OK to freeze
protect from light
kolor
light beige
rozpuszczalność
DMSO: 50 mg/mL
temp. przechowywania
−20°C
Opis ogólny
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.
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).
Działania biochem./fizjol.
Cell permeable: yes
Primary Target
RIPK2
RIPK2
Ostrzeżenie
Toxicity: Standard Handling (A)
Rekonstytucja
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Inne uwagi
Tigno-Aranjuez, J.T., et al. 2014. J. Biol. Chem.289, 29651.
Informacje prawne
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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Kod klasy składowania
11 - Combustible Solids
Klasa zagrożenia wodnego (WGK)
WGK 3
Temperatura zapłonu (°F)
Not applicable
Temperatura zapłonu (°C)
Not applicable
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