WEHI-345 – 1 mg

Brand:
Cayman
CAS:
1354825-58-3
Storage:
-20
UN-No:
Non-Hazardous - /

WEHI-345 is an inhibitor of receptor-interacting protein kinase 2 (RIPK2; IC50 = 130 nM in a kinase assay using human recombinant RIPK2).{41305} It is selective for RIPK2 over RIPK1, 4, and 5 (Kds = 46, >10,000, >10,000, and >10,000 nM, respectively) and a panel of 95 kinases at a concentration of 1 μM. WEHI-345 reduces levels of RIPK2 phosphorylation at Ser176 in bone marrow-derived macrophages (BMDMs) stimulated by muramyl dipeptide (MDP). It decreases MDP-induced transcription of TNF and IL-6 in BMDMs and reduces mRNA levels of the NF-κB target genes TNF, IL-8, IL-1β, and A20 in MDP-stimulated THP-1 cells in a concentration-dependent manner. WEHI-345 (3-10 mg/kg) reduces plasma levels of TNF and delays disease onset in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

 

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SKU: 23023 - 1 mg Category:

Description

An inhibitor of RIPK2 (IC50 = 130 nM in a kinase assay using human recombinant RIPK2); selective for RIPK2 over RIPK1, 4, and 5 (Kds = 46, >10,000, >10,000, and >10,000 nM, respectively) and a panel of 95 kinases at a concentration of 1 μM; reduces levels of RIPK2 phosphorylation at Ser176 in MDP-stimulated BMDMs; decreases MDP-induced transcription of TNF and IL-6 in BMDMs and reduces mRNA levels of the NF-κB target genes TNF, IL-8, IL-1β, and A20 in MDP-stimulated THP-1 cells in a concentration-dependent manner; reduces plasma levels of TNF and delays disease onset in a mouse model of EAE when administered at doses ranging from 3-10 mg/kg


Formal name: N-[2-[4-amino-3-(4-methylphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-2-methylpropyl]-4-pyridinecarboxamide

Synonyms: 

Molecular weight: 401.5

CAS: 1354825-58-3

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|NF-κB Signaling||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation|Autoimmunity||Research Area|Immunology & Inflammation|Innate Immunity