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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.

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  1. Cat.No. Product Name Information
  2. 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.
  3. 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.
  4. 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.
  5. B1130 GLPG0634 GLPGGLPG0634 is a selective inhibitor of JAK1 with IC50 value of 10nM .
  6. A4514 NSC 33994 Selective inhibitor of JAK2 (IC50 = 60 nM).
  7. 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.
  8. A4516 TCS 21311 Potent JAK3 inhibitor (IC50 = 8 nM). Selective for JAK3 over JAK1, JAK2 and TYK2 (IC50 values are 1017, 2550 and 8055 nM respectively). Also inhibits GSK-3β, PKCα and PKCθ (IC50 values are 3, 13 and 68 nM respectively).
  9. A4515 SD 1008 JAK2/STAT3 signaling pathway inhibitor. Inhibits activation of STAT3, JAK2 and Src. Induces apoptosis in cell lines expressing constitutively active tyrosine-phosphorylated STAT3.
  10. 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.
  11. A4512 Cucurbitacin I Selective inhibitor of STAT3/JAK2 signaling. Inhibits the activation of STAT3 and JAK2 and displays no activity on Src, Akt, ERK and JNK. Suppresses phosphotyrosine levels of STAT3, inhibits STAT3 DNA binding and STAT3-mediated gene expression. Induces apoptosis in cell lines expressing constitutively active tyrosine-phosphorylated STAT3.

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