JAK - Selective
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.
- B1130 GLPG06341 Citation中文名: 菲戈替尼Target: JAKSummary: JAK1抑制剂
- A4512 Cucurbitacin I中文名: 葫芦素 ITarget: STAT|JAKSummary: STAT3/JAK2信号转导抑制剂
- A3937 XL019Target: JAKSummary: 有效的JAK2选择性抑制剂
- 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
- A4148 NVP-BSK805 2HClTarget: JAKSummary: JAK2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
- 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