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Tyk2-IN-3
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Tyk2-IN-3图片
CAS NO:1779493-12-7
包装与价格：
包装价格(元)
250mg电议
500mg电议

产品介绍
Tyk2-IN-3是Tyk2pseudokinase的一个抑制剂，其IC50值为485nM。
Cas No.1779493-12-7
Canonical SMILESCN1C=NC2=C1C(N=C(C3=CC=CC([C@@H](C)NC(C4=C(S(=O)(C)=O)C=CC=C4)=O)=C3)S5)=C5N=C2NC
分子式C25H24N6O3S2
分子量520.63
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.