Cas No.: | 1354825-58-3 |
Chemical Name: | WEHI345,WEHI 345 |
Synonyms: | WEHI345,WEHI 345 |
SMILES: | CC1=CC=C(C=C1)C2=NN(C3=C2C(=NC=N3)N)C(C)(C)CNC(=O)C4=CC=NC=C4 |
Formula: | C22H23N7O |
M.Wt: | 401.46 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | WEHI-345 is a potent and selective inhibitor of RIPK2, with IC50 of 0.13 μM. |
In Vivo: | WEHI-345 inhibits NOD signalling and has a beneficial effect on an EAE model. WEHI-345 blocks MDP-induced cytokine production. WEHI-345 ameliorates experimental autoimmune encephalomyelitis in mice. WEHI-345 also potently inhibited MDP-induced cytokine and chemokine secretion in the mouse macrophage Raw 264.7 cell line. |
In Vitro: | WEHI-345 is a selective RIPK2 kinase inhibitor, which delays RIPK2 ubiquitylation and NF-κB activation downstream of NOD engagement. WEHI-345 is an ATP analogue and was therefore predicted to bind in the ATP-binding pocket of RIPK2. WEHI-345 proved to be highly specific for RIPK2(Kd=46 nM) and displayed negligible activity (>10 μM) against RIPK1, RIPK4 and RIPK5. |