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Home >> Signaling Pathways >> JAK/STAT Signaling >> 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. GC34971 (3R,4S)-Tofacitinib (3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. (3R,4S)-Tofacitinib Chemical Structure
  3. GC34972 (3S,4R)-Tofacitinib (3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. (3S,4R)-Tofacitinib Chemical Structure
  4. GC34973 (3S,4S)-Tofacitinib (3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. (3S,4S)-Tofacitinib Chemical Structure
  5. GC63864 (E/Z)-Zotiraciclib hydrochloride (E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor. (E/Z)-Zotiraciclib hydrochloride Chemical Structure
  6. GC32023 Abrocitinib (PF-04965842) Abrocitinib (PF-04965842) (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) Chemical Structure
  7. GC32028 BMS-066 BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. BMS-066 Chemical Structure
  8. 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. Brepocitinib (PF-06700841) Chemical Structure
  9. GC35554 Brevilin A A sesquiterpene lactone with anticancer activity Brevilin A Chemical Structure
  10. GC11209 Cerdulatinib (PRT062070) Cerdulatinib (PRT062070) (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively. Cerdulatinib (PRT062070) Chemical Structure
  11. GC11652 CHZ868 Type II JAK2 inhibitor CHZ868 Chemical Structure
  12. GC31660 Delgocitinib (JTE-052) Delgocitinib (JTE-052) (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Delgocitinib (JTE-052) Chemical Structure
  13. GC16875 FLLL32 STAT3 inhibitor FLLL32 Chemical Structure
  14. GC19408 FM381

    FM-381 is a highly potent and JAK3-selective janus kinase (JAK) inhibitor

     FM381 Chemical Structure
  15. GC68378 GDC-4379 GDC-4379 Chemical Structure
  16. GC12579 GLPG0634 GLPG0634 (GLPG0634) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. GLPG0634 Chemical Structure
  17. GC17222 GLPG0634 analogue GLPG0634 analogue (Compoun 176) is a broad spectrum JAK inhibitor with IC50 values of <100 nM against JAK1, JAK2 and JAK3. GLPG0634 analogue Chemical Structure
  18. GC33041 Gusacitinib (ASN-002) Gusacitinib (ASN-002) (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Gusacitinib (ASN-002) has anti-cancer activity in both solid and hematological tumor types. Gusacitinib (ASN-002) Chemical Structure
  19. GC64108 Ifidancitinib Ifidancitinib (ATI-50002) is a potent and selective inhibitor of JAK kinases 1/3. Ifidancitinib Chemical Structure
  20. GC32809 Ilginatinib (NS-018) Ilginatinib (NS-018) (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). Ilginatinib (NS-018) Chemical Structure
  21. GC33037 Ilginatinib hydrochloride (NS-018 hydrochloride) Ilginatinib hydrochloride (NS-018 hydrochloride) (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). Ilginatinib hydrochloride (NS-018 hydrochloride) Chemical Structure
  22. GC33018 Ilginatinib maleate (NS-018 (maleate)) Ilginatinib maleate (NS-018 (maleate)) (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). Ilginatinib maleate (NS-018 (maleate)) Chemical Structure
  23. GC19204 Itacitinib Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis. Itacitinib Chemical Structure
  24. GC36351 Itacitinib adipate Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis. Itacitinib adipate Chemical Structure
  25. GC31866 JAK inhibitor 1 JAK inhibitor 1 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283. JAK inhibitor 1 Chemical Structure
  26. GC31999 JAK-IN-1 JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 Chemical Structure
  27. GC36366 JAK-IN-10 JAK-IN-10 is a JAK inhibitor. JAK-IN-10 Chemical Structure
  28. GC68000 JAK-IN-23 JAK-IN-23 Chemical Structure
  29. GC65453 JAK-IN-3 JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively. JAK-IN-3 Chemical Structure
  30. GC64959 JAK/HDAC-IN-1 JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively. JAK/HDAC-IN-1 Chemical Structure
  31. GC33036 JAK1-IN-3 JAK1-IN-3 (AZD4205) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM). JAK1-IN-3 Chemical Structure
  32. GC33258 JAK1-IN-4 JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM). JAK1-IN-4 Chemical Structure
  33. GC36363 JAK1-IN-7 JAK1-IN-7 (JAK1-IN-7) is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect. JAK1-IN-7 Chemical Structure
  34. GC36364 JAK2-IN-4 JAK2-IN-4 (compound 16h) is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively. JAK2-IN-4 Chemical Structure
  35. GC65405 JAK2-IN-6 JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells. JAK2-IN-6 Chemical Structure
  36. GC36365 JAK3 covalent inhibitor-1 JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs. JAK3 covalent inhibitor-1 Chemical Structure
  37. GC33046 JAK3-IN-1 JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM). JAK3-IN-1 Chemical Structure
  38. GC31902 JAK3-IN-6 JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM. JAK3-IN-6 Chemical Structure
  39. GC33382 JAK3-IN-7 JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC50 of <0.01 μM. JAK3-IN-7 Chemical Structure
  40. GC14857 LFM-A13 BTK-specific tyrosine kinase inhibitor LFM-A13 Chemical Structure
  41. GC64372 Lorpucitinib Lorpucitinib is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease. Lorpucitinib Chemical Structure
  42. GC36646 Momelotinib Mesylate Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3. Momelotinib Mesylate Chemical Structure
  43. GC66329 NDI-034858 NDI-034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM. NDI-034858 Chemical Structure
  44. GC36783 NVP-BSK805 dihydrochloride A potent, selective JAK2 inhibitor NVP-BSK805 dihydrochloride Chemical Structure
  45. GC31677 Oclacitinib maleate (PF-03394197 maleate) Oclacitinib maleate (PF-03394197 maleate) (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) Chemical Structure
  46. GC41329 Pacritinib FMS-like tyrosine kinase 3 (FLT3) and Janus kinase 2 (JAK2) are tyrosine kinases that mediate cytokine signaling and are frequently mutated in cancers, particularly acute myeloid leukemia. Pacritinib Chemical Structure
  47. GC10341 Peficitinb (ASP015K, JNJ-54781532) Peficitinb (ASP015K, JNJ-54781532) (ASP015K) is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Peficitinb (ASP015K, JNJ-54781532) Chemical Structure
  48. GC14938 PF-03394197(Oclacitinib) Novel Janus kinase inhibitor PF-03394197(Oclacitinib) Chemical Structure
  49. GC36882 PF-06263276 PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. PF-06263276 Chemical Structure
  50. GC19288 PF-06651600 PF-06651600 (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM. PF-06651600 Chemical Structure
  51. GC19405 PF-06700841 P-Tosylate Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. PF-06700841 P-Tosylate Chemical Structure
  52. GC64701 Povorcitinib Povorcitinib is a potent and selective inhibitor of JAK1. Povorcitinib Chemical Structure
  53. GC64700 Povorcitinib phosphate Povorcitinib phosphate Chemical Structure
  54. GC30601 Propanamide Propanamide is a potent and selective JAK inhibitor extracted from patent WO2012122452A1, Compound II, has the potential for the skin disorders (such as cutaneous lupus) treatment. Propanamide Chemical Structure
  55. GC34742 Protosappanin A

    Protosappanin A (PTA), an immunosuppressive ingredient and major biphenyl compound isolated from Caesalpinia sappan L, suppresses JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3.

     Protosappanin A Chemical Structure
  56. GC69780 Pumecitinib

    Pumecitinib is a JAK inhibitor with anti-inflammatory activity.

     Pumecitinib Chemical Structure
  57. GC37522 RGB-286638 A multi-kinase inhibitor RGB-286638 Chemical Structure
  58. GC37523 RGB-286638 free base A multi-kinase inhibitor RGB-286638 free base Chemical Structure
  59. GC25869 RO495 RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2). RO495 Chemical Structure
  60. 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
  61. 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
  62. 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
  63. GC25992 TG-89 TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM. TG-89 Chemical Structure
  64. 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
  65. GC32052 Tyk2-IN-3 Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM. Tyk2-IN-3 Chemical Structure
  66. 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
  67. 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
  68. 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
  69. 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
  70. 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
  71. GC67867 VVD-118313 VVD-118313 Chemical Structure
  72. 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
  73. 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

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