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JAK

Inhibitory Selectivity

Catalog No.Inhibitor Name JAK1JAK2JAK3Tyk2Other
A11041Ruxolitinib
***
****
A10241Tofacitinib Citrate
**
**
****
ROCK2,LCK
A10110AZD1480
****
A11082Fedratinib
****
FLT3,RET
A10095AT9283
****
****
***
Aurora B,Aurora A,Abl1
A10047AG-490
*
EGFR,ErbB2
A10263Momelotinib
***
***
*
A11795WP1066
*
STAT3
A11180TG101209
***
*
RET,FLT3
A10546Gandotinib
**
****
**
**
FLT3,FLT4,FGFR2
A11193NVP-BSK805 2HCl
**
****
***
***
A11329Baricitinib
***
***
**
A10104AZ 960
****
A12808CEP-33779
****
A12694Pacritinib
*
**
*
**
FLT3 (D835Y),FLT3
A14049WHI-P154
*
EGFR,Src,VEGFR
A12394XL019
*
****
*
*
PDGFRβ,FLT3,c-Kit
A14955S-Ruxolitinib
***
****
*
**
A13509ZM 39923 HCl
*
*
TGM2,EGFR
A14012Decernotinib
***
***
****
***
A14210Cerdulatinib
***
***
***
****
ARK5,MST1,Fms
A14232Filgotinib
***
**
*
*
A15911FLLL32
*
A11241BMS-911543
*
****
**
**
A14438Peficitinib
A13162GLPG0634 analogue
A12419Go6976
FLT3,PKCα,PKCβ1
A10247Curcumol
A11608WHI-P97
A13082PF-03394197 (oclacitinib)
***
***
**
**
A13457Pyridone 6 (JAK Inhibitor I)
***
****
****
A14132NSC 42834(JAK2 Inhibitor V, Z3)
A14390INCB39110 (Itacitinib)
A14405Solcitinib (GSK2586184)
A15134JANEX-1
*
A15362Cercosporamide
***
Mnk2, Mnk1
A15365TCS 21311
*
*
***
*
A15366ZM 449829
****
****
STAT-5, EGFR, CDK4
A15389NSC 33994
A16227ZM 39923
*
*
TGM2, EGFR

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

产品 1 到 50 共 88个

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  1. Decernotinib
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    Decernotinib

    Catalog No. A14012
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    JAK3 抑制剂
    Decernotinib是Vertex开发的口服选择性Janus激酶3（JAK3）抑制剂。 了解更多
  2. ZM 39923 HCl
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    ZM 39923 HCl

    Catalog No. A13509
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    JAK3 抑制剂
    ZM 39923 HCl是JAK3抑制剂（IC50 = 79 nM），其抑制表皮生长因子受体，JAK1和细胞周期蛋白依赖性激酶4（IC50s分别为2.4、40和10 M）的抑制作用较小。 了解更多
  3. S-Ruxolitinib
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    S-Ruxolitinib

    Catalog No. A14955
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    JAK 抑制剂
    S-Ruxolitinib是INCB018424的手性化合物，是一种有效且选择性的小分子Janus激酶1（JAK1）和JAK2抑制剂。 了解更多
  4. CYT387 sulfate salt
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    CYT387 sulfate salt

    Catalog No. A15056
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    JAK 抑制剂
    CYT387 sulfate salt是JAK1/JAK2的ATP竞争性抑制剂，IC50为11 nM/18 nM，是JAK3的约10倍选择性。 了解更多
  5. JANEX-1
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    JANEX-1

    Catalog No. A15134
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    JAK3 抑制剂
    Janex-1是JAK3的细胞渗透性，可逆性，有效，ATP竞争性和特异性抑制剂（IC50 = 78 uM）；对JAK1，JAK2或Zap/Syk或SRC酪氨酸激酶无影响。 了解更多
  6. 1,2,3,4,5,6-Hexabromocyclohexane
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    1,2,3,4,5,6-Hexabromocyclohexane

    Catalog No. A15361
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    JAK2 抑制剂
    1,2,3,4,5,6-Hexabromocyclohexane是一种有效且特异性的JAK2自磷酸化抑制剂。 了解更多
  7. Cercosporamide
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    Cercosporamide

    Catalog No. A15362
    Mnk2/JAK3 抑制剂
    Cercosporamide是一种USnic酰胺，最初在Cercosporidium henningsii中被鉴定为宿主选择性植物毒素和广谱抗真菌剂，并且是MAP激酶相互作用激酶2（Mnk2；IC50 = 11 nM），JAK3（IC50 = 31）和Mnk1（IC50 = 116 nM）。 了解更多
  8. Cucurbitacin I
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    Cucurbitacin I

    Catalog No. A15363
    JAK2/STAT3 抑制剂
    Cucurbitacin I（Cucumis sativus L.）可以抑制v-Src转化的NIH 3T3细胞中的磷酸酪氨酸Stat3（信号转导和转录激活因子3）水平。 了解更多
  9. SD 1008
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    SD 1008

    Catalog No. A15364
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    JAK2/STAT3 抑制剂
    SD 1008是JAK2/STAT3信号通路抑制剂，可额外抑制Src。注意到SD 1008可诱导表达组成性活性酪氨酸磷酸化STAT3的细胞系凋亡。 了解更多
  10. TCS 21311
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    TCS 21311

    Catalog No. A15365
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    JAK3 抑制剂
    TCS 21311是有效的JAK3抑制剂（IC50 = 8 nM）。TCS 21311对于JAK3相对于JAK1，JAK2和Tyk 2具有选择性（IC50值分别为1017、2550和8055 nM）。 了解更多
  11. ZM 449829
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    ZM 449829

    Catalog No. A15366
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    JAK/STAT 抑制剂
    ZM 449829是有效的、选择性的JAK3抑制剂（Janus酪氨酸激酶3），与JAK3 ATP位点竞争性结合。 了解更多
  12. NSC 33994
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    NSC 33994

    Catalog No. A15389
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    JAK2 抑制剂
    NSC 33994是JAK2酪氨酸激酶（Janus激酶2）的新型抑制剂。Janus激酶2（JAK2）在骨髓增生性疾病和血液系统恶性肿瘤的发病机制中起着至关重要的作用。 了解更多
  13. Peficitinib (ASP015K, JNJ-54781532)
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    Peficitinib (ASP015K, JNJ-54781532)

    Catalog No. A14438
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    JAK 抑制剂?
    Peficitinib (ASP015K,JNJ-54781532)是一种新型的强力JAK抑制剂，在佐剂诱导的大鼠关节炎模型中显示出强效功效。 了解更多
  14. FLLL32
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    FLLL32

    Catalog No. A15911
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    JAK2 抑制剂
    FLLL32是一种有效的JAK2/STAT3双重抑制剂，IC50 <5 uM。 了解更多
  15. WHI-P97
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    WHI-P97

    Catalog No. A11608
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    JAK3 抑制剂
    WHI-P97是合理设计的JAK-3抑制剂。 了解更多
  16. NS-018
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    NS-018

    Catalog No. A16224
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    JAK2 抑制剂
    NS-018是Janus相关激酶2（JAK2）和Src家族激酶的口服生物利用型小分子抑制剂，具有潜在的抗肿瘤活性。 了解更多
  17. NS-018 hydrochloride
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    NS-018 hydrochloride

    Catalog No. A16225
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    JAK2 抑制剂
    NS-018 hydrochloride是一种新型的高选择性JAK2抑制剂。 了解更多
  18. NS-018 maleate
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    NS-018 maleate

    Catalog No. A16226
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    JAK2 抑制剂
    NS-018 maleate是在Ba/F3-JAK2V617F细胞中具有ATP竞争性的JAK2小分子抑制剂，IC50为470nM。与其他JAK家族激酶（例如JAK1，JAK3和酪氨酸激酶2）相比，对JAK2的选择性高30-50倍。 了解更多
  19. ZM39923
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    ZM39923

    Catalog No. A16227
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    JAK1/3 抑制剂
    ZM39923是一种JAK1/3抑制剂，pIC50为4.4/7.1，对JAK2几乎没有活性，对EGFR的作用中等。还发现对转谷氨酰胺酶敏感。 了解更多
  20. AZ-3
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    AZ-3

    Catalog No. A19217
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    JAK1 inhibitor
    AZ-3 is a potent and selective JAK1 inhibitor with an IC50 of 34 nM. 了解更多
  21. Delgocitinib
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    Delgocitinib

    Catalog No. A19234
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    JAK inhibitor
    Delgocitinib is a novel and specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. 了解更多
  22. JAK1-IN-3
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    JAK1-IN-3

    Catalog No. A19251
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    JAK1 inhibitor
    JAK1-IN-3 is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC50, >14.7, >30 μM, respectively). 了解更多
  23. JAK-IN-5
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    JAK-IN-5

    Catalog No. A19792
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    JAK inhibitor
    JAK-IN-5 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283. 了解更多
  24. Gusacitinib
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    Gusacitinib

    Catalog No. A19883
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    SYK/JAK inhibitor
    Gusacitinib (ASN-002) is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. 了解更多
  25. FM381
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    FM381

    Catalog No. A20138
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    JAK3 inhibitor
    FM381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909 at the gatekeeper position +7 in JAK3. 了解更多
  26. JAK-IN-3
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    JAK-IN-3

    Catalog No. A20220
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    JAK inhibitor
    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. 了解更多
  27. JAK-IN-4
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    JAK-IN-4

    Catalog No. A20230
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    JAK inhibitor
    JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model. 了解更多
  28. SAR-20347
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    SAR-20347

    Catalog No. A20380
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    TYK2/JAK1/JAK2/JAK3 inhibitor
    SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively. 了解更多
  29. JAK3-IN-1
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    JAK3-IN-1

    Catalog No. A20734
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    JAK3 inhibitor
    JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM). 了解更多
  30. INCB018424 (Ruxolitinib)
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    INCB018424 (Ruxolitinib)

    Catalog No. A11041
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    JAK1/2 抑制剂
    INCB018424 (Ruxolitinib)是有效和选择性的Janus相关激酶JAK1/2抑制剂，对JAK1，JAK2和JAK3的IC50分别为2.7、4.5和332 nM。 了解更多
  31. AT9283
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    AT9283

    Catalog No. A10095
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    Aurora/JAK 抑制剂
    AT9283抑制极光激酶A和B，并靶向与骨髓细胞增殖相关的其他酪氨酸和丝氨酸/苏氨酸激酶。 了解更多
  32. AG-490
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    AG-490

    Catalog No. A10047
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    EGFR 抑制剂
    AG 490是EGF受体酪氨酸激酶的选择性抑制剂 (EGFR和ErbB2的IC50值分别为2和13.5μM)。也抑制对Lck，Lyn，Btk，Syk和Src无活性的JAK2。 了解更多
  33. CP-690550 (Tofacitinib citrate)
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    CP-690550 (Tofacitinib citrate)

    Catalog No. A10241
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    JAK3 抑制剂
    CP-690550 (Tofacitinib citrate)是口服的高选择性Janus激酶（JAK）酶抑制剂。 了解更多
  34. Cyt387 (Momelotinib)
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    Cyt387 (Momelotinib)

    Catalog No. A10263
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    JAK 抑制剂
    Cyt387 (Momelotinib)是Janus激酶JAK1和JAK2的抑制剂，可作为ATP竞争者，IC50值分别为11和18 nM。 了解更多
  35. Curcumol
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    Curcumol

    Catalog No. A10247
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    JAK2 抑制剂
    Curcumol是常见的传统中药，具有抗肿瘤活性。 了解更多
  36. Pacritinib (SB1518)
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    Pacritinib (SB1518)

    Catalog No. A12694
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    JAK2/FLT3 抑制剂
    Pacritinib (SB1518)是Janus激酶2（JAK2）和JAK2突变体JAK2V617F的口服生物利用抑制剂，无细胞试验中IC50分别为23和22 nM，具有潜在的抗肿瘤活性。Pacritinib与JAK2竞争ATP结合，这可能导致抑制JAK2活化，抑制JAK-STAT信号传导途径以及半胱天冬酶依赖性凋亡。 了解更多
  37. PF-03394197 (oclacitinib)
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    PF-03394197 (oclacitinib)

    Catalog No. A13082
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    JAK1 抑制剂
    PF-03394197 (oclacitinib)是有效的JAK1抑制剂。 了解更多
  38. GLPG0634
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    GLPG0634

    Catalog No. A13162
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    JAK1 抑制剂
    GLPG0634是一种口服的JAK1(Janus激酶1)选择性抑制剂，对 JAK1/JAK2/JAK3的IC50值为50-200 nM。用于治疗类风湿性关节炎和潜在的其他炎性疾病。 了解更多
  39. Solcitinib (GSK2586184)
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    Solcitinib (GSK2586184)

    Catalog No. A14405
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    JAK1 抑制剂
    Solcitinib (GSK2586184)是Janus激酶1（JAK1）抑制剂。 了解更多
  40. INCB39110 (Itacitinib)
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    INCB39110 (Itacitinib)

    Catalog No. A14390
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    JAK1 抑制剂
    INCB39110 (Itacitinib)是一种有效的JAK1酪氨酸激酶抑制剂，目前正在II期试验中，用于治疗类风湿关节炎，骨髓纤维化，类风湿关节炎和斑块状牛皮癣。 了解更多
  41. Filgotinib
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    Filgotinib

    Catalog No. A14232
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    JAK 抑制剂
    Filgotinib是一种选择性的JAK1抑制剂，对于JAK1，JAK2，JAK3和TYK2的IC50分别为10 nM，28 nM，810 nM和116 nM。 了解更多
  42. PRT 062070 (Cerdulatinib)
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    PRT 062070 (Cerdulatinib)

    Catalog No. A14147
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    Dual Syk and JAK 抑制剂
    PRT 062070 (Cerdulatinib)是一种新型的口服双脾酪氨酸激酶（Syk）和janus激酶（JAK）抑制剂。Cerdulatinib优先抑制各种细胞类型中JAK1和JAK3依赖性细胞因子介导的信号传导和功能性反应。 了解更多
  43. NSC 42834(JAK2 Inhibitor V, Z3)
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    NSC 42834(JAK2 Inhibitor V, Z3)

    Catalog No. A14132
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    JAK2 抑制剂
    NSC 42834(JAK2 Inhibitor V,Z3)是一种新型的Jak2酪氨酸激酶特异性抑制剂。 了解更多
  44. JAK1-IN-4
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    JAK1-IN-4

    Catalog No. A18821
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    JAK1 抑制剂
    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). 了解更多
  45. Tofacitinib
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    Tofacitinib

    Catalog No. A17252
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    JAK3/2/1 inhibitor
    Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively. 了解更多
  46. PF-06263276
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    PF-06263276

    Catalog No. A12572
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    pan-JAK inhibitor
    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. 了解更多
  47. Ruxolitinib sulfate
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    Ruxolitinib sulfate

    Catalog No. A11467
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    JAK1/2 inhibitor
    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. 了解更多
  48. JAK2-IN-4
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    JAK2-IN-4

    Catalog No. A12182
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    JAK2/JAK3 inhibitor
    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. 了解更多
  49. JAK/HDAC-IN-1
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    JAK/HDAC-IN-1

    Catalog No. A13362
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    JAK2/HDAC dual inhibitor
    JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. 了解更多
  50. Oclacitinib maleate
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    Oclacitinib maleate

    Catalog No. A16640
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    JAK inhibitor
    Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC50=10 nM). 了解更多

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作用机制
  1. Inhibitor (抑制剂) (78)
靶点
  1. Aurora A (1)
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  5. EGFR (2)
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  8. JAK1 (18)
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  13. PKCα (1)
  14. PKCβ (1)
  15. RET (1)
  16. STAT1 (1)
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