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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.

  1. Cat.No. 产品名称 Information
  2. GC25992 TG-89 TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM.
  3. GC25869 RO495 RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2).
  4. GC25168 Brepocitinib (PF-06700841) Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.
  5. GC67867 VVD-118313
  6. GC66329 NDI-034858
  7. GC65453 JAK-IN-3
  8. GC65405 JAK2-IN-6
  9. GC65387 Tyk2-IN-5
  10. GC64959 JAK/HDAC-IN-1
  11. GC64701 Povorcitinib
  12. GC64700 Povorcitinib phosphate
  13. GC64372 Lorpucitinib
  14. GC64108 Ifidancitinib
  15. GC63864 (E/Z)-Zotiraciclib hydrochloride
  16. GC63448 JAK-IN-14
  17. GC63416 Itacnosertib
  18. GC63309 Ilunocitinib
  19. GC63029 JAK1-IN-8
  20. GC62908 Coumermycin A1
  21. GC62665 JAK2/FLT3-IN-1 TFA
  22. GC62500 JAK2-IN-7
  23. GC62491 BMS-986202
  24. GC62313 Izencitinib
  25. GC62246 G5-7 G5-7 is an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2.
  26. GC62233 2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide A TYK2 inhibitor
  27. GC62130 (2R,5S)-Ritlecitinib
  28. GC62112 Zotiraciclib Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency.
  29. GC61807 (E/Z)-AG490
  30. GC50480 PF 06651600 malonate Potent and selective JAK3 inhibitor
  31. GC50066 Atiprimod dihydrochloride JAK2 inhibitor
  32. GC39081 Reticuline
  33. GC37971 ZM39923 A potent inhibitor of JAK3
  34. GC37847 Tyk2-IN-8 Ropsacitinib (PF-06826647, Tyk2-IN-8, compound 10) is a selective and orally administered inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 17 nM for binding to TYK2 catalytically active JH1 domain. PF-06826647 (Tyk2-IN-8, compound 10) also inhibits JAK1 and JAK2 with IC50 of 383 nM and 74 nM, respectively. PF-06826647 (Tyk2-IN-8, compound 10) is used in the treatment of psoriasis (PSO).
  35. GC37846 Tyk2-IN-7
  36. GC37575 Ruxolitinib sulfate A potent, selective JAK1/JAK2 inhibitor
  37. GC37523 RGB-286638 free base A multi-kinase inhibitor
  38. GC37522 RGB-286638 A multi-kinase inhibitor
  39. GC36882 PF-06263276
  40. GC36783 NVP-BSK805 dihydrochloride A potent, selective JAK2 inhibitor
  41. GC36646 Momelotinib Mesylate
  42. GC36366 JAK-IN-10
  43. GC36365 JAK3 covalent inhibitor-1
  44. GC36364 JAK2-IN-4
  45. GC36363 JAK1-IN-7
  46. GC36351 Itacitinib adipate A JAK1 inhibitor
  47. GC35554 Brevilin A A sesquiterpene lactone with anticancer activity
  48. GC34973 (3S,4S)-Tofacitinib
  49. GC34972 (3S,4R)-Tofacitinib
  50. GC34971 (3R,4S)-Tofacitinib
  51. GC43406 Delphinidin (chloride) Natural vasorelaxant and inhibitor of EGFRs and HATs

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