5.32757

RIPK2 Inhibitor, OD36

• 동의어(들): RIPK2 Inhibitor, OD36, RIPK2 inhibitor, RIP kinase inhibitor
• 실험식(Hill 표기법): C₁₆H₁₅ClN₄O₂
• CAS Number: 1638644-62-8
• Molecular Weight: 330.77
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥97% (HPLC)
• Quality Level: 100
• 형태: powder
• 효능: 5.3 nM IC₅₀
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: light beige
• solubility: DMSO: 50 mg/mL
• 저장 온도: −20°C

설명

일반 설명

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).

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
RIPK2

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

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