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.
- 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
- A4143 CYT3871 Citation中文名: 莫莫替尼Summary: JAK-1/-2抑制剂
- A4141 Baricitinib (LY3009104, INCB028050)2 Citation中文名: 巴瑞克替尼Summary: 可口服的JAK1/JAK2抑制剂
- A4140 WP1066Target: STAT|JAKSummary: 细胞通透的JAK2/STAT3抑制剂。
- A4138 Tofacitinib (CP-690550,Tasocitinib)1 Citation中文名: 托法替尼,托法替布Target: JAKSummary: Janus激酶抑制剂
- A4137 AZD1480Target: JAKSummary: 新型的ATP竞争性JAK2抑制剂
- A4136 TG101348 (SAR302503)2 Citation中文名: 费德拉替尼Target: FLT3|JAK|c-RETSummary: JAK-2抑制剂
- A4135 Tofacitinib (CP-690550) Citrate2 Citation中文名: 托法替尼Target: JAKSummary: JAK抑制剂