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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.

Products for  JAK

  1. Cat.No. Product Name Information
  2. GC72769 (1R)-AZD-1480 (1R)-AZD-1480 is the (1R) chiral isomer of AZD-1480, an ATP competitive JAK1 and JAK2 inhibitor. (1R)-AZD-1480  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. GC63864 (E/Z)-Zotiraciclib hydrochloride

    (E/Z)-TG02 hydrochloride; (E/Z)-SB1317 hydrochloride

    (E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor. (E/Z)-Zotiraciclib hydrochloride  Chemical Structure
  7. GC32023 Abrocitinib (PF-04965842)

    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
  8. GC32028 BMS-066 BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. BMS-066  Chemical Structure
  9. GC25168 Brepocitinib (PF-06700841)

    PF-841

    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
  10. GC35554 Brevilin A

    6-O-Angeloylprenolin, Brevelin A

    A sesquiterpene lactone with anticancer activity Brevilin A  Chemical Structure
  11. GC68819 Butyzamide

    Butyzamide is an orally effective Mpl activator, where Mpl is a receptor for thrombopoietin (TPO) involved in platelet production. Butyzamide increases the phosphorylation levels of JAK2, STAT3, STAT5 and MAPK. In mouse xenograft experiments, Butyzamide increases human platelet levels.

    Butyzamide  Chemical Structure
  12. GC11209 Cerdulatinib (PRT062070)

    PRT062070, PRT2070

    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
  13. GC11652 CHZ868 Type II JAK2 inhibitor CHZ868  Chemical Structure
  14. 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
  15. GC71575 Deuruxolitinib Deuruxolitinib, a deuterated Ruxolitinib , modulates the activity of JAK1/JAK2. Deuruxolitinib  Chemical Structure
  16. GC16875 FLLL32

    JAK2 Inhibitor X

    STAT3 inhibitor FLLL32  Chemical Structure
  17. GC19408 FM381

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

    FM381  Chemical Structure
  18. GC70307 Fosifidancitinib Fosifidancitinib is a potent and selective inhibitor of JAK kinases 1/3. Fosifidancitinib  Chemical Structure
  19. GC68378 GDC-4379 GDC-4379  Chemical Structure
  20. GC12579 GLPG0634

    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
  21. 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
  22. GC69190 GS-829845

    GS-829845 is the main active metabolite of Filgotinib. It is a JAK1 inhibitor, but its potency is about 10 times lower than that of the parent compound and it has a longer half-life.

    GS-829845  Chemical Structure
  23. GC33041 Gusacitinib (ASN-002)

    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
  24. GC73627 HDAC/JAK/BRD4-IN-1 HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1  Chemical Structure
  25. GC64108 Ifidancitinib

    ATI-50002; ATI-502

    Ifidancitinib (ATI-50002) is a potent and selective inhibitor of JAK kinases 1/3. Ifidancitinib  Chemical Structure
  26. GC32809 Ilginatinib (NS-018)

    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
  27. GC33037 Ilginatinib hydrochloride (NS-018 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
  28. GC33018 Ilginatinib maleate (NS-018 (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
  29. GC19204 Itacitinib

    INCB 039110

    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
  30. GC36351 Itacitinib adipate

    INCB039110 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
  31. GC72815 Itacnosertib (hydrocholide)

    TP-0184 (hydrocholide

    Itacnosertib drocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5. Itacnosertib (hydrocholide)  Chemical Structure
  32. GC70213 JAK 3i JAK3i is a highly selective JAK3 inhibitor (IC50: 0.43 nM). JAK 3i  Chemical Structure
  33. GC31866 JAK inhibitor 1 JAK inhibitor 1 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283. JAK inhibitor 1  Chemical Structure
  34. 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
  35. GC36366 JAK-IN-10 JAK-IN-10 is a JAK inhibitor. JAK-IN-10  Chemical Structure
  36. GC73148 JAK-IN-21 JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively. JAK-IN-21  Chemical Structure
  37. GC68000 JAK-IN-23 JAK-IN-23  Chemical Structure
  38. GC71213 JAK-IN-24 JAK-IN-24 is a JAK inhibitor, with IC50s of 0.534 and 24 nM at the presence of 4 μM or 1mM ATP, respectively. JAK-IN-24  Chemical Structure
  39. GC69306 JAK-IN-25

    JAK-IN-25 (compound 19) is an effective JAK inhibitor with IC50 values of 6 nM, 21 nM, 8 nM, and 1051 nM for TYK2, JAK1, JAK2, and JAK3 respectively. It inhibits human whole blood IL-12 (HEB IL-12) with an IC50 value of 28 nM. JAK-IN-25 has potential for use in cancer research.

    JAK-IN-25  Chemical Structure
  40. GC73475 JAK-IN-26 JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics. JAK-IN-26  Chemical Structure
  41. 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
  42. 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
  43. GC73456 JAK1-IN-11 JAK1-IN-11 (compound 11) is a potent inhibitor of JAK,with IC50s of 0.02 nM (JAK1),and 0.44 nM (JAK2),respectively. JAK1-IN-11  Chemical Structure
  44. GC71475 JAK1-IN-13 JAK1-IN-13 (compound 36b) is an orally active, potent and highly selective inhibitor of JAK1 with an IC50 of 0.044 nM. JAK1-IN-13  Chemical Structure
  45. GC33036 JAK1-IN-3

    Golidocitinib; AZD4205

    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
  46. 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
  47. GC36363 JAK1-IN-7

    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
  48. 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
  49. 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
  50. GC69305 JAK2/FLT3-IN-1

    JAK2/FLT3-IN-1 is an orally effective 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. It has anti-cancer activity.

    JAK2/FLT3-IN-1  Chemical Structure
  51. 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
  52. 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
  53. GC73600 JAK3-IN-14 JAK3-IN-14 (compound 1) is a potent JAK3 inhibitor, with IC50 values of 38 and 600 nM for JAK3 and JAK2, respectively. JAK3-IN-14  Chemical Structure
  54. 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
  55. 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
  56. GC71392 Lepzacitinib Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3. Lepzacitinib  Chemical Structure
  57. GC14857 LFM-A13 BTK-specific tyrosine kinase inhibitor LFM-A13  Chemical Structure
  58. GC64372 Lorpucitinib

    JNJ-64251330

    Lorpucitinib is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease. Lorpucitinib  Chemical Structure
  59. GC36646 Momelotinib Mesylate

    CYT387 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
  60. GC66329 NDI-034858 NDI-034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM. NDI-034858  Chemical Structure
  61. GC71049 Nimucitinib Nimucitinib is a Janus kinase (JAK) inhibitor. Nimucitinib  Chemical Structure
  62. GC36783 NVP-BSK805 dihydrochloride A potent, selective JAK2 inhibitor NVP-BSK805 dihydrochloride  Chemical Structure
  63. 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
  64. 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
  65. GC10341 Peficitinb (ASP015K, JNJ-54781532)

    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
  66. GC14938 PF-03394197(Oclacitinib)

    PF-03394197

    Novel Janus kinase inhibitor PF-03394197(Oclacitinib)  Chemical Structure
  67. 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
  68. GC19288 PF-06651600

    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
  69. GC19405 PF-06700841 P-Tosylate

    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
  70. GC64701 Povorcitinib

    INCB54707

    Povorcitinib is a potent and selective inhibitor of JAK1. Povorcitinib  Chemical Structure
  71. GC64700 Povorcitinib phosphate Povorcitinib phosphate  Chemical Structure
  72. 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
  73. GC71201 PROTAC TYK2 degradation agent1 PROTAC TYK2 degradation agent1 is a potent and subtype-selective TYK2 degrader. PROTAC TYK2 degradation agent1  Chemical Structure
  74. 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
  75. GC69780 Pumecitinib

    Pumecitinib is a JAK inhibitor with anti-inflammatory activity.

    Pumecitinib  Chemical Structure
  76. GC37522 RGB-286638 A multi-kinase inhibitor RGB-286638  Chemical Structure
  77. GC37523 RGB-286638 free base A multi-kinase inhibitor RGB-286638 free base  Chemical Structure
  78. GC70211 Ritlecitinib tosylate Ritlecitinib tosylate is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM. Ritlecitinib tosylate  Chemical Structure
  79. GC25869 RO495

    CS-2667

    RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2). RO495  Chemical Structure
  80. 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
  81. 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
  82. GC73139 SJ1008030 formic SJ1008030 (compound 8) formic is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 formic  Chemical Structure
  83. GC73369 SJ988497 SJ988497 is a PROTAC JAK2 degrader. SJ988497  Chemical Structure
  84. GC19334 Solcitinib

    GLPG0778, GSK2586184

    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
  85. GC25992 TG-89 TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM. TG-89  Chemical Structure
  86. 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
  87. GC32052 Tyk2-IN-3 Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM. Tyk2-IN-3  Chemical Structure
  88. GC31659 Tyk2-IN-4 (BMS-986165)

    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
  89. 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
  90. 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
  91. 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
  92. GC19368 Upadacitinib

    ABT-494

    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
  93. GC67867 VVD-118313 VVD-118313  Chemical Structure
  94. 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
  95. 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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