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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. 产品名称 Information
  2. GC19368 Upadacitinib

    乌帕替尼; ABT-494

     A JAK1 inhibitor
  3. GC19334 Solcitinib

    索西替尼; GSK-2586184; GLPG-0778

     A JAK1 inhibitor
  4. GC19320 SAR-20347 A JAK family kinase inhibitor
  5. GC19288 PF-06651600

    PF-06651600

     PF-06651600 (PF-06651600) 是一种具有口服活性的选择性 JAK3 抑制剂，IC50 为 33.1 nM。
  6. GC19204 Itacitinib

    伊他替尼,INCB039110

     A JAK1 inhibitor
  7. GC10341 Peficitinb (ASP015K, JNJ-54781532)

    培菲替尼,ASP015K; JNJ-54781532

     A JAK inhibitor
  8. GC16875 FLLL32

    (2E,2'E)-1,1'-环己基亚基二[3-(3,4-二甲氧基苯基)-2-丙烯-1-酮]

     An inhibitor of JAK2/STAT3 signaling
  9. GC11652 CHZ868 CHZ868 是一种 II 型 JAK2 抑制剂，在 EPOR JAK2 WT Ba/F3 细胞中的 IC50 为 0.17 μM。
  10. GC14938 PF-03394197(Oclacitinib)

    奥拉替尼

     A JAK family kinase inhibitor
  11. GC10770 Decernotinib(VX-509)

    迪西替尼

     A selective JAK3 inhibitor
  12. GC14857 LFM-A13 A BTK inhibitor
  13. GC11209 Cerdulatinib (PRT062070)

    赛度替尼,PRT062070; PRT2070

     A dual inhibitor of Syk and JAKs
  14. GC17222 GLPG0634 analogue GLPG0634 类似物 (Compoun 176) 是一种广谱 JAK 抑制剂，对 JAK1、JAK2 和 JAK3 的 IC50 值 <100 nM。
  15. GC12579 GLPG0634

    非戈替尼,GLPG0634

     A JAK1 inhibitor
  16. GC14676 Pacritinib (SB1518)

    帕克替尼

     An equipotent inhibitor of FLT3 and JAK2
  17. GC17762 NSC 33994 NSC 33994 (G6) 是一种选择性 JAK2 抑制剂，IC50 为 60 nM。
  18. GC15125 ZM 449829

    2-萘乙烯基酮

     An inhibitor of JAK3
  19. GC16584 TCS 21311

    NIBR3049

     A JAK3 inhibitor
  20. GC12118 SD 1008

    SD 1008 是一种有效的 JAK 抑制剂。 SD 1008 抑制 STAT3、JAK2 和 Src 的酪氨酰磷酸化。 SD 1008 还降低 STAT3 依赖性荧光素酶活性。 SD 1008 通过直接阻断 JAK-STAT3 信号通路增强紫杉醇诱导的卵巢癌细胞凋亡。
  21. GC17033 Lestaurtinib

    来他替尼; CEP-701; KT-5555

     A potent JAK2 and PRK1 kinase inhibitor
  22. GC13347 Cucurbitacin I

    葫芦素I,Elatericin B; JSI-124; NSC-521777

     An inhibitor STAT3/JAK signaling
  23. GC15391 Cercosporamide

    尾孢素酰胺,(-)-Cercosporamide

    A potent inhibitor of fungal Pkc1 and mammalian Mnk isoforms
  24. GC17055 1,2,3,4,5,6-Hexabromocyclohexane

    1,2,3,4,5,6-六溴化环己烷

     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。
  25. GC14327 XL019

    XL-019;XL 019

     A potent, bioavailable JAK2 inhibitor
  26. GC15956 WHI-P97

    4-(3',5'-二溴-4-羟基苯基)氨基-6,7-二甲氧基喹唑啉,WHI-P-97;WHI P97

     WHI-P97 是一种有效的选择性 JAK-3 抑制剂。
  27. GC12064 SB1317

    14-甲基-20-氧杂-5,7,14,27-四氮杂四环[19.3.1.1(2,6).1(8,12)]二十七碳-1(25),2,4,6(27),8,10,12(26),16,21,23-十烯,TG02;SB 1317;TG 02;SB-1317;TG-02

     A multi-kinase inhibitor
  28. GC16124 Ruxolitinib phosphate

    鲁索利替尼磷酸盐,INCB018424 phosphate;INCB 018424 phosphate;INCB-018424 phosphate;Ruxolitinib

     A potent and selective JAK1/JAK2 inhibitor
  29. GC11525 Pyridone 6

    吡啶酮6

     吡啶酮 6 抑制 Jak3，K(I)=5 nM； Pyridone 6 还抑制 Jak 家族成员 Tyk2 和 Jak2，IC(50)=1 nM 和 Jak1，IC(50)=15 nM。
  30. GC13229 NVP-BSK805

    BSK 805;BSK-805;BSK805;NVP-BSK 805

    A potent, selective JAK2 inhibitor
  31. GC14671 JANEX-1

    4-(4'-羟基苯基)氨基-6,7-二甲氧基喹唑啉,WHI-P131;Janex 1;WHI-P 131

     A selective JAK3 inhibitor
  32. GC13826 JAK2 Inhibitor V, Z3

    Z3; NSC 42834;1-Butanone, 2-methyl-1-phenyl-4-(2-pyridinyl)-2-[2-(2-pyridinyl)ethyl]-

     A selective inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK
  33. GC16468 CYT387 sulfate salt

    N-(氰基甲基)-4-[2-[[4-(4-吗啉基)苯基]氨基]-4-嘧啶基]苯甲酰胺硫酸盐(1:2),CYT-387 sulfate;CYT 387 sulfate

     A potent inhibitor of JAK1 and JAK2
  34. GC13830 Baricitinib phosphate

    磷酸巴瑞克替尼; LY3009104 phosphate; INCB028050 phosphate

     A JAK1 and JAK2 inhibitor
  35. GC11572 Bardoxolone methyl

    甲基巴多索隆; RTA 402; NSC 713200; CDDO Methyl ester

     A synthetic triterpenoid with potent anticancer and antidiabetic activity
  36. GC12454 BMS-911543 A potent, selective JAK2 inhibitor
  37. GC10638 AT9283 A broad spectrum kinase inhibitor
  38. GC14245 ZM 39923 HCl

    3-[异丙基(苄基)氨基]-1-(2-萘基)-1-丙酮盐酸盐

     A potent inhibitor of JAK3
  39. GC15589 WHI-P154

    2-溴-4-(6,7-二甲氧基喹唑啉-4-基氨基)苯酚

     A JAK3 inhibitor
  40. GC17020 S-Ruxolitinib (INCB018424)

    S-鲁索替尼,S-Ruxolitinib; INCB18424

     鲁索替尼 S 对映体是鲁索替尼的 S 对映体。鲁索替尼 S 对映异构体是一种 JAK 抑制剂
  41. GC13848 LY2784544

    Gandotinib

     Potent inhibitor of JAK2
  42. GC12083 CEP-33779

    N-[3-(4-甲基-1-哌嗪基)苯基]-8-[4-(甲磺酰基)苯基]-[1,2,4]三唑并[1,5-A]吡啶-2-胺,CEP 33779,CEP33779

     A potent, orally available inhibitor of JAK2
  43. GC10035 TG101209

    N-(1,1-二甲基乙基)-3-[[5-甲基-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-4-嘧啶基]氨基]苯磺酰胺,TG-101209

     An inhibitor of JAK2, FLT3, RET, and JAK3
  44. GC13433 AZ 960

    5-氟-2-[[(1S)-1-(4-氟苯基)乙基]氨基]-6-[(5-甲基-1H-吡唑-3-基)氨基]-3-吡啶腈,AZ-960,AZ960

     A JAK2 inhibitor
  45. GC17050 CYT387

    莫洛替尼,Cyt-387,MOMELOTINIB,CYT 387,CYT 11387

     A potent inhibitor of JAK1 and JAK2
  46. GC14844 Baricitinib (LY3009104, INCB028050)

    巴瑞替尼; LY3009104; INCB028050

     A JAK1 and JAK2 inhibitor
  47. GC15980 WP1066

    (2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基乙基]-2-丙烯酰胺

    An inhibitor of STAT3
  48. GC16828 Tofacitinib (CP-690550,Tasocitinib)

    托法替尼; Tasocitinib; CP-690550

     Tofacitinib (CP-690550,Tasocitinib) 是一种口服的 JAK3/2/1 抑制剂，IC50 分别为 1、20 和 112 nM。
  49. GC12504 AZD1480

    5-氯-N2-[(1S)-1-(5-氟-2-嘧啶基)乙基]-N4-(5-甲基-1H-吡唑-3-基)-2,4-嘧啶二胺,AZD 1480

     A potent JAK2 inhibitor
  50. GC14324 TG101348 (SAR302503)

    N-(1,1-二甲基乙基)-3-[[5-甲基-2-[[4-[2-(1-吡咯烷基)乙氧基]苯基]氨基]-4-嘧啶基]氨基]苯磺酰胺,Tg-101348,SAR-302503

     A JAK2 inhibitor
  51. GC17586 Tofacitinib (CP-690550) Citrate

    枸橼酸托法替尼; Tasocitinib citrate; CP-690550 citrate

     A pan-JAK inhibitor

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