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TCS 21311
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。
TCS 21311图片
CAS NO:1260181-14-3
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
TCS 21311 (NIBR3049) 是一种有效的、高选择性的 JAK3 抑制剂，IC50 为 8 nM，其选择性是 JAK1、JAK2 和 TYK2 的 100 倍以上。 TCS 21311 (NIBR3049) 抑制 PKCα、PKCθ 和 GSK3β，IC50 分别为 13、68 和 3 nM。
Cas No.1260181-14-3
别名NIBR3049
化学名3-[5-[4-(2-hydroxy-2-methylpropanoyl)piperazin-1-yl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)pyrrole-2,5-dione
Canonical SMILESCC(C)(C(=O)N1CCN(CC1)C2=CC(=C(C=C2)C(F)(F)F)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54)O
分子式C27H25F3N4O4
分子量526.51
溶解度<52.65mg/ml in DMSO
储存条件Desiccate at RT
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

TCS 21311 is a potent and selective JAK3 inhibitor with the IC50 values of 8 nM. TCS 21311 shows high selectivity for JAK3 over JAK1, JAK2 and TYK2. The IC50 values are 1017, 2550 and 8055 nM respectively. TCS 21311 exihibits inhibitory effect on GSK-3β, PKCα and PKCθ with the IC50 values of 3, 13 and 68 nM, respectively [1].

Janus kinases (JAK) belong to a small family of cytoplasmic protein tyrosine kinases including JAK1, JAK2, Tyk2, and JAK3, which play important roles in initiating the cytokine-triggered signaling events by activators of transcription (STAT) proteins via tyrosine phosphorylation [2]. Due to its association with relevant cytokine signaling pathways, JAK3 serves as an important target for therapeutic intervention in the treatment of inflammatory diseases, autoimmune disorders and organ transplant rejection [2].

References:
[1] Thoma G, Nuninger F, Falchetto R, et al.  Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family[J]. Journal of medicinal chemistry, 2010, 54(1): 284-288.
[2] Clark M P, George K M, Bookland R G, et al.  Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3)[J]. Bioorganic & medicinal chemistry letters, 2007, 17(5): 1250-1253.