Tyk2-IN-3
Names
[ CAS No. ]:
1779493-12-7
[ Name ]:
Tyk2-IN-3
Biological Activity
[Description]:
Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM.
[Related Catalog]:
[Target]
Tyk2:485 nM (IC50)
[In Vivo]
Tyk2-IN-3 (compound 1) is very potent against the Tyk2 pseudokinase (99% inhibition at 1 μM) but lacks potency against all other kinases in the kinome assay panel except IKK (96% inhibition) and the JAK1 pseudokinase domain (99% inhibition at 1 μM). No evidence of binding to the catalytic domain of Tyk2 or any other JAK family kinase is evident at 1 μM, and subsequent enzymatic assays confirm the lack of activity against purified catalytic domains (IC50>>2 μM). The pseudokinase domains of JAK2 and JAK3 are not part of the kinome screening panel. In the IL-23-stimulated kit225 T cell assay, Tyk2-IN-3 inhibits the stimulated response with an IC50 of 485±143 nM (n=3)[1].
[References]
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Chemical & Physical Properties
[ Molecular Formula ]:
C25H24N6O3S2
[ Molecular Weight ]:
520.63