JAK
Janus kinases (JAKs), belonging to a distinct family of tyrosine kinases, are non-receptor tyrosine kinases that transduce signals of cytokine receptors via diverse signal transduction pathways. Mammalian JAK family consists of four structurally similar members, JAK1, JAK2, JAK3 and Tyrosine kinase 2 (TYK2), which are characterized by containing seven JAK homology (JH) domains. The presence of JH1 and JH2 domains is the most intriguing feature of JAK proteins. JH1 domain is the main catalytic domain; while JH2 is usually considered as a catalytically inactive pseudokinase domain. However, results of recent studies have shown that JH2 acts as a dual-specificity protein kinase to phosphorylate two regulatory sites (Ser523 and Tyr570) in JAK2.
- A3221 Bardoxolone methyl中文名: 甲基巴多索隆Target: Nrf2Summary: IKK抑制剂,强效的抗氧化炎性反应调节剂。
- A4152 BMS-911543Target: JAKSummary: JAK2抑制剂
- A4151 ZM 39923 HClTarget: JAKSummary: 有效的JAK3选择性抑制剂
- A4150 WHI-P154Target: VEGFR|Src|EGFR|JAKSummary: JAK3抑制剂
- A4149 S-Ruxolitinib (INCB018424)中文名: 鲁索替尼Target: JAKSummary: JAK1/2抑制剂
- A4148 NVP-BSK805 2HClTarget: JAKSummary: JAK2抑制剂
- A4147 LY2784544Target: Aurora Kinases|FLT3|VEGFR|FGFR|Trk Receptors|JAK|ALK|TYK2|MUSK|MAP3KSummary: JAK2抑制剂
- A4146 CEP-337791 CitationSummary: 具高度选择性的JAK2抑制剂。
- A4145 TG101209Summary: JAK2/3抑制剂
- A4144 AZ 960Target: JAKSummary: JAKs(janus相关激酶)抑制剂