1779493-12-7

1779493-12-7 structure
1779493-12-7 structure
  • Name: Tyk2-IN-3
  • Chemical Name: Tyk2-IN-3
  • CAS Number: 1779493-12-7
  • Molecular Formula: C25H24N6O3S2
  • Molecular Weight: 520.63
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2019-02-09 20:31:02
  • Modify Date: 2024-01-10 18:09:20
  • Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM.

Name Tyk2-IN-3
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

[1]. Tokarski JS, et al. Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain. J Biol Chem. 2015 Apr 24;290(17):11061-74.

Molecular Formula C25H24N6O3S2
Molecular Weight 520.63