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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. GC62130 (2R,5S)-Ritlecitinib (2R,5S)-Ritlecitinib ((2R,5S)-PF-06651600) is a potent and selective JAK3 inhibitor (IC50=144.8 nM) extracted from patent US20150158864A1, example 68. (2R,5S)-Ritlecitinib Chemical Structure
  3. GC34971 (3R,4S)-Tofacitinib (3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. (3R,4S)-Tofacitinib Chemical Structure
  4. GC34972 (3S,4R)-Tofacitinib (3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. (3S,4R)-Tofacitinib Chemical Structure
  5. GC34973 (3S,4S)-Tofacitinib (3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. (3S,4S)-Tofacitinib Chemical Structure
  6. GC61807 (E/Z)-AG490 (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3. (E/Z)-AG490 Chemical Structure
  7. 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
  8. GC17055 1,2,3,4,5,6-Hexabromocyclohexane 1,2,3,4,5,6-六溴环己烷（1,2,3,4,5,6-Hexabromocyclohexane）直接抑制JAK2激酶结构域内的口袋，抑制自身磷酸化。 1,2,3,4,5,6-Hexabromocyclohexane Chemical Structure
  9. GC62233 2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively. 2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide Chemical Structure
  10. GC46503 2-(1,8-Naphthyridin-2-yl)phenol 2-(1,8-Naphthyridin-2-yl)phenol is a selective enhancer of STAT1 transcription. 2-(1,8-Naphthyridin-2-yl)phenol can enhance the ability of IFN-γ to inhibit the proliferation of human breast cancer and fibrosarcoma cells. 2-(1,8-Naphthyridin-2-yl)phenol Chemical Structure
  11. 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
  12. GC10638 AT9283 A broad spectrum kinase inhibitor AT9283 Chemical Structure
  13. GC50066 Atiprimod dihydrochloride JAK2 inhibitor Atiprimod dihydrochloride Chemical Structure
  14. GN10627 Atractylenolide I Atractylenolide I Chemical Structure
  15. GC13433 AZ 960 A JAK2 inhibitor AZ 960 Chemical Structure
  16. GC12504 AZD1480 A potent JAK2 inhibitor AZD1480 Chemical Structure
  17. GC11572 Bardoxolone methyl A synthetic triterpenoid with potent anticancer and antidiabetic activity Bardoxolone methyl Chemical Structure
  18. GC14844 Baricitinib (LY3009104, INCB028050) A JAK1 and JAK2 inhibitor Baricitinib (LY3009104, INCB028050) Chemical Structure
  19. GC13830 Baricitinib phosphate A JAK1 and JAK2 inhibitor Baricitinib phosphate Chemical Structure
  20. GC32028 BMS-066 BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. BMS-066 Chemical Structure
  21. GC12454 BMS-911543 A potent, selective JAK2 inhibitor BMS-911543 Chemical Structure
  22. GC62491 BMS-986202 BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM. BMS-986202 Chemical Structure
  23. 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
  24. GC35554 Brevilin A A sesquiterpene lactone with anticancer activity Brevilin A Chemical Structure
  25. GC12083 CEP-33779 A potent, orally available inhibitor of JAK2 CEP-33779 Chemical Structure
  26. 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
  27. GC11652 CHZ868 Type II JAK2 inhibitor CHZ868 Chemical Structure
  28. GC62908 Coumermycin A1

    Coumermycin A1 is a JAK2 signal activator.

     Coumermycin A1 Chemical Structure
  29. GN10442 Curculigoside Curculigoside Chemical Structure
  30. GC17050 CYT387 A potent inhibitor of JAK1 and JAK2 CYT387 Chemical Structure
  31. GC16468 CYT387 sulfate salt A potent inhibitor of JAK1 and JAK2 CYT387 sulfate salt Chemical Structure
  32. GC10770 Decernotinib(VX-509) Decernotinib(VX-509) is a potent, orally active JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively. Decernotinib(VX-509) Chemical Structure
  33. 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
  34. GC43406 Delphinidin (chloride)

    Delphinidin (chloride) is an anthocyanidin, a natural plant pigment which serves as the precursor of certain anthocyanins that provide the blue-red colors of flowers, fruits, and red wine.

     Delphinidin (chloride) Chemical Structure
  35. GC46148 Filgotinib-d4 An internal standard for the quantification of filgotinib Filgotinib-d4 Chemical Structure
  36. GC16875 FLLL32 STAT3 inhibitor FLLL32 Chemical Structure
  37. GC19408 FM381

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

     FM381 Chemical Structure
  38. GC62246 G5-7 G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study. G5-7 Chemical Structure
  39. GC68378 GDC-4379 GDC-4379 Chemical Structure
  40. GN10584 Ginsenoside Rk1 Ginsenoside Rk1 Chemical Structure
  41. 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
  42. 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
  43. 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
  44. GC64108 Ifidancitinib Ifidancitinib (ATI-50002) is a potent and selective inhibitor of JAK kinases 1/3. Ifidancitinib Chemical Structure
  45. GC47450 IL-4 Inhibitor IL-4 Inhibitor (compound 52) is an IL-4 inhibitor, with an EC50 of 1.81 μM. IL-4 Inhibitor Chemical Structure
  46. 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
  47. 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
  48. 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
  49. GC63309 Ilunocitinib Ilunocitinib (compound 27) is a JAK inhibitor (extracted from patent WO2009114512A1). Ilunocitinib Chemical Structure
  50. 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
  51. 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
  52. GC63416 Itacnosertib Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871. Itacnosertib Chemical Structure
  53. GC62313 Izencitinib Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. Izencitinib Chemical Structure
  54. GC31866 JAK inhibitor 1 JAK inhibitor 1 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283. JAK inhibitor 1 Chemical Structure
  55. 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
  56. GC36366 JAK-IN-10 JAK-IN-10 is a JAK inhibitor. JAK-IN-10 Chemical Structure
  57. GC63448 JAK-IN-14 JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM. JAK-IN-14 Chemical Structure
  58. GC68000 JAK-IN-23 JAK-IN-23 Chemical Structure
  59. 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
  60. 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
  61. 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
  62. 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
  63. 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
  64. GC63029 JAK1-IN-8 JAK1-IN-8, a potent JAK1 inhibitor (IC50<500 nM), compound 28, extracted from patent WO2016119700A1. JAK1-IN-8 Chemical Structure
  65. GC13826 JAK2 Inhibitor V, Z3 A selective inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK JAK2 Inhibitor V, Z3 Chemical Structure
  66. 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
  67. 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
  68. GC62500 JAK2-IN-7 JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities. JAK2-IN-7 Chemical Structure
  69. GC62665 JAK2/FLT3-IN-1 TFA JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity. JAK2/FLT3-IN-1 TFA Chemical Structure
  70. 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
  71. 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
  72. 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
  73. 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
  74. GC14671 JANEX-1 A selective JAK3 inhibitor JANEX-1 Chemical Structure
  75. GC14857 LFM-A13 BTK-specific tyrosine kinase inhibitor LFM-A13 Chemical Structure
  76. GC64372 Lorpucitinib Lorpucitinib is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease. Lorpucitinib Chemical Structure
  77. GC13848 LY2784544 Potent inhibitor of JAK2 LY2784544 Chemical Structure
  78. 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
  79. GC40791 MS-1020 MS-1020 is a cell-permeable inhibitor of janus kinase 3 (JAK3), strongly inhibiting constitutive autophosphorylation of JAK3 in L540 cells when used at 30-50 μM. MS-1020 Chemical Structure
  80. GC66329 NDI-034858 NDI-034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM. NDI-034858 Chemical Structure
  81. GC17762 NSC 33994 Selective inhibitor of JAK2 (IC50 = 60 nM). Displays no effect on Src and TYK2 tyrosine kinase activity at a concentration of 25 μM. NSC 33994 Chemical Structure
  82. GC13229 NVP-BSK805

    A potent, selective JAK2 inhibitor

     NVP-BSK805 Chemical Structure
  83. GC36783 NVP-BSK805 dihydrochloride A potent, selective JAK2 inhibitor NVP-BSK805 dihydrochloride Chemical Structure
  84. 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
  85. 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
  86. 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
  87. GC50480 PF 06651600 malonate Potent and selective JAK3 inhibitor PF 06651600 malonate Chemical Structure
  88. GC14938 PF-03394197(Oclacitinib) Novel Janus kinase inhibitor PF-03394197(Oclacitinib) Chemical Structure
  89. 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
  90. 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
  91. 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
  92. GC64701 Povorcitinib Povorcitinib is a potent and selective inhibitor of JAK1. Povorcitinib Chemical Structure
  93. GC64700 Povorcitinib phosphate Povorcitinib phosphate Chemical Structure
  94. 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
  95. 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
  96. GC69780 Pumecitinib

    Pumecitinib is a JAK inhibitor with anti-inflammatory activity.

     Pumecitinib Chemical Structure
  97. GC11525 Pyridone 6 A pan-JAK inhibitor Pyridone 6 Chemical Structure
  98. GC39081 Reticuline Reticuline shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline Chemical Structure
  99. GC37522 RGB-286638 A multi-kinase inhibitor RGB-286638 Chemical Structure
  100. GC37523 RGB-286638 free base A multi-kinase inhibitor RGB-286638 free base Chemical Structure
  101. GC25869 RO495 RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2). RO495 Chemical Structure

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