TK-453 (TK453) is a potent, selective SHP2 allosteric inhibitor with IC50 of 18.76 and 179 nM for SHP2-WT and SHP2-E76K, respectively.TK-453 has strong inhibitory effect on the enzyme activity of the SHP2-WT, and does not inhibit the activity of the SHP2-PTP catalytic domain, and homologues (SHP1 and PTP1B).TK-453 binds SHP2-WT (KD=150 nM) and SHP2-E76K, higher affinity with SHP2 than SHP099.TK-453 binds in the allosteric binding pocket at the junction of three domains and stabilizes the autoinhibition conformation of SHP2.TK-453 alleviates imiquimod (IMQ)-induced inflammation in macrophages, inhibits the phosphorylation levels of p-IKKα/β and p-p65.TK-453 significantly ameliorates imiquimod-triggered skin-like inflammation in mice via inhibition of IL-23/Th17 axis.
Cat.No
DC70848
Name
TK-453
Chemical Properties
CAS
1801692-60-3
Formula
C17H21CL2N5S
MW
398.35
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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