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Home >> Signaling Pathways >> Chromatin/Epigenetics >> JAK

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.

Products for  JAK

  1. Cat.No. Product Name Information
  2. GC14191 Ruxolitinib (INCB018424)

    Ruxolitinib (INCB018424), as an inhibitor, inhibits Janus-associated kinases (JAKs)JAK1 and JAK2 with IC50 values of 3.3 nM and 2.8 nM, respectively.

     Ruxolitinib (INCB018424) Chemical Structure
  3. GC16124 Ruxolitinib phosphate A potent and selective JAK1/JAK2 inhibitor Ruxolitinib phosphate Chemical Structure
  4. GC37575 Ruxolitinib sulfate Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib sulfate Chemical Structure
  5. GC17020 S-Ruxolitinib (INCB018424) S-Ruxolitinib (INCB018424) Chemical Structure
  6. GC19320 SAR-20347 SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively. SAR-20347 Chemical Structure
  7. GC12064 SB1317 A multi-kinase inhibitor SB1317 Chemical Structure
  8. GC19334 Solcitinib Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis. Solcitinib Chemical Structure
  9. GC25992 TG-89 TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM. TG-89 Chemical Structure
  10. GC10035 TG101209 An inhibitor of JAK2, FLT3, RET, and JAK3 TG101209 Chemical Structure
  11. GC14324 TG101348 (SAR302503) A JAK2 inhibitor TG101348 (SAR302503) Chemical Structure
  12. GC17586 Tofacitinib (CP-690550) Citrate A pan-JAK inhibitor Tofacitinib (CP-690550) Citrate Chemical Structure
  13. GC16828 Tofacitinib (CP-690550,Tasocitinib) Tofacitinib (CP-690550,Tasocitinib) Chemical Structure
  14. GC49692 Tofacitinib-d3 (citrate) An internal standard for the quantification of tofacitinib Tofacitinib-d3 (citrate) Chemical Structure
  15. GC31668 TYK2-IN-2 TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TYK2-IN-2 Chemical Structure
  16. GC32052 Tyk2-IN-3 Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM. Tyk2-IN-3 Chemical Structure
  17. GC31659 Tyk2-IN-4 (BMS-986165) Tyk2-IN-4 (BMS-986165) (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Tyk2-IN-4 (BMS-986165) Chemical Structure
  18. GC65387 Tyk2-IN-5 Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Tyk2-IN-5 Chemical Structure
  19. GC37846 Tyk2-IN-7 Tyk2-IN-7 (Compound 48) is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki. Tyk2-IN-7 Chemical Structure
  20. GC37847 Tyk2-IN-8 Tyk2-IN-8 (Compound 3) is a selective Tyk-2 inhibitor with an IC50 of 5.7 nM for TYK2-JH2. Tyk2-IN-8 Chemical Structure
  21. GC19368 Upadacitinib Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders. Upadacitinib Chemical Structure
  22. GC67867 VVD-118313 VVD-118313 Chemical Structure
  23. GC40761 VX-509 VX-509 is a selective inhibitor of Janus kinase 3 (JAK3) with a Ki value of 2.5 nM in enzyme assays and an IC50 value of 50-170 nM in cellular assays dependent on JAK3 activity with no measurable activity against other JAK isotypes. VX-509 Chemical Structure
  24. GC15589 WHI-P154 A JAK3 inhibitor WHI-P154 Chemical Structure
  25. GC15956 WHI-P97 WHI-P97 Chemical Structure
  26. GC15980 WP1066

    An inhibitor of STAT3

     WP1066 Chemical Structure
  27. GC14327 XL019 A potent, bioavailable JAK2 inhibitor XL019 Chemical Structure
  28. GC14245 ZM 39923 HCl A potent inhibitor of JAK3 ZM 39923 HCl Chemical Structure
  29. GC15125 ZM 449829 An inhibitor of JAK3 ZM 449829 Chemical Structure
  30. GC37971 ZM39923 ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM. ZM39923 Chemical Structure
  31. GC62112 Zotiraciclib Zotiraciclib Chemical Structure

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