TCS 21311 是一种高选择性JAK3抑制剂,IC50为 8 nM,它的选择性是 JAK1、JAK2 和 TYK2 的100倍以上,还抑制PKCα、PKCθ和GSK3β,IC50值分别为 13、68 和 3 nM。
产品描述
TCS 21311 is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectively). It displays >100-fold selectivity over JAK1, JAK2, and TYK2.
体外活性
TCS 21311 displays moderate activity in this cellular assay (IC50=689 nM, Jurkat cells), which is in good agreement with its enzymatic Pkc activity. TCS 21311 shows IC50 values of 1.017, 2.550, and 8.055 μM for JAK1, JAK2, and TYK2, respectively?in an enzymatic Jak assay [1].
Cas No.
1260181-14-3
分子式
C27H25F3N4O4
分子量
526.51
别名
NIBR3049
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years