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.
- Cat.No. Product Name Information
- B1259 (3R,4S)-Tofacitinib Tasocitinib also known as CP690550 is an JAK kinase inhibitor. An IC50 estimated at 0.2 μM for PV patient progenitor cells.
- B1031 (3S,4S)-Tofacitinib Tasocitinib also known as CP690550 is an JAK kinase inhibitor. An IC50 estimated at 0.2 μM for PV patient progenitor cells.
- B1258 (3S,4R)-Tofacitinib Tasocitinib also known as CP690550 is an JAK kinase inhibitor. An IC50 estimated at 0.2 μM for PV patient progenitor cells.
- B1130 GLPG0634 GLPGGLPG0634 is a selective inhibitor of JAK1 with IC50 value of 10nM .
- A4517 ZM 449829 Potent, selective inhibitor of Janus tyrosine kinase 3 (JAK3) which binds competitively to the JAK3 ATP site. pIC50 values are 6.8, 5.0, 4.7, and < 5.0 for JAK3, EGFR, JAK1 and CDK4 respectively.
- A4513 Lestaurtinib Potent JAK2, FLT3 and TrkA inhibitor (IC50 values are 0.9, 3 and < 25 nM respectively) that prevents STAT5 phosphorylation (IC50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro (IC50 = 30 - 100 nM in HEL92.1.7 cells) and is effective against myeloproliferative disorders in vivo.
BMS-911543 is a selective small-molecule inhibitor of JAK2 with IC50 value of 1.1nM .
- A4151 ZM 39923 HCl ZM 39923 is a selective inhibitor of JAK1 and JAK3 with pIC50 value of 4.4 and 7.1, respectively  .
- A4150 WHI-P154 WHI-P154 is an inhibitor of JAK3 with IC50 value of 1.8μM .
NVP-BSK805 is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM,>20-fold selectivity towards JAK1, JAK3 and TYK2.