5.32757

RIPK2 Inhibitor, OD36

• 別名: RIPK2 Inhibitor, OD36, RIPK2 inhibitor, RIP kinase inhibitor
• 実験式（ヒル表記法）: C₁₆H₁₅ClN₄O₂
• CAS番号: 1638644-62-8
• 分子量: 330.77
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥97% (HPLC)
• 品質水準: 100
• 形状: powder
• 有効性: 5.3 nM IC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: light beige
• 溶解性: DMSO: 50 mg/mL
• 保管温度: −20°C

詳細

詳細

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).

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
RIPK2

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable