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  • Tyk2-IN-3
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Tyk2-IN-3

Tyk2-IN-3是Tyk2pseudokinase的一个抑制剂,其IC50值为485nM。

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  • 货号: ajcx12744
  • CAS: 1779493-12-7
  • 别名:
  • 分子式: C25H24N6O3S2
  • 分子量: 520.63
  • 纯度: >98%
  • 溶解度: Soluble in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM.


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].


[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.

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