JAK

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 79个

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  1. 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
  2. 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
  3. 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
  4. 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
  5. 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
  6. JAK3 covalent inhibitor-1

    Catalog No. A18926
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    JAK3 covalent 抑制剂
    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. 了解更多
  7. JAK1-IN-7

    Catalog No. A19029
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    JAK1 抑制剂
    JAK1-IN-7 is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect. 了解更多
  8. TG-02 (SB1317)

    Catalog No. A11962
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    FLT3 抑制剂
    TG-02 (SB1317)是一种新型的小分子有效CDK/JAK2/FLT3抑制剂。 了解更多
  9. Tyk2-IN-8

    Catalog No. A19052
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    TYK2 抑制剂
    Tyk2-IN-8 (compound 10) is a selective TYK2 inhibitor, which binds to TYK2 catalytically active JH1 domain with an IC50 of 17 nM, used in the treatment of psoriasis. 了解更多
  10. BMS-986165

    Catalog No. A18726
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    TYK2 抑制剂
    BMS-986165 is a Highly Potent and Selective Allosteric Inhibitor of TYK2. BMS-986165 Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease. 了解更多
  11. Upadacitinib (ABT-494)

    Catalog No. A18316
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    JAK-1 抑制剂
    Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders with an IC50 of 43 nM. IC50 & Target: IC50: 43 nM (JAK1), 200 nM (JAK2) 了解更多
  12. WHI-P258

    Catalog No. A18317
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    JAK3 抑制剂
    WHI-P258 is a quinazoline compound that modeling studies suggested would bind to the active site of JAK3 with an estimated Ki value of 72 uM. 了解更多
  13. Abrocitinib (PF-04965842)

    Catalog No. A18318
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    JAK1 抑制剂
    Abrocitinib (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) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease. 了解更多
  14. JAK3-IN-2

    Catalog No. A18323
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    JAK3 抑制剂
    JAK3-IN-2 is a potent and highly selective JAK3 inhibitor with IC50 of 0.15 nM. dispalys >4,300-fold selectivity over JAK1, JAK2 and TYK2, and other kinases BMX, EGFR, ITK and BTK; blocks cytokine signaling through JAK3, but not through other JAK family enzymes; inhibits IL-7 induced pSTAT5 in CD3+, CD8+ T cells with IC50 of 280 nM; sufficiently blocks the development of inflammation in a rat model of rheumatoid arthritis, while sparing hematopoiesis. 了解更多
  15. PF-06700841 tosylate

    Catalog No. A17176
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    JAK1 and TYK2 抑制剂
    PF-06700841 tosylate是JAK1和TYK2激酶的抑制剂。 了解更多
  16. Ruxolitinib Phosphate

    Catalog No. A11552
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    JAK 抑制剂
    Ruxolitinib Phosphate是ruxolitinib的磷酸盐形式,ruxolitinib是一种口服生物可利用的Janus相关激酶(JAK)抑制剂,具有潜在的抗肿瘤和免疫调节活性。 了解更多
  17. PF-06651600

    Catalog No. A16803
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    JAK3 抑制剂
    PF-06651600是一种有效且不可逆的JAK3选择性抑制剂,IC50为33.1 nM,但对JAK1,JAK2和TYK2没有活性(IC50> 10 000 nM)。 了解更多
  18. CHZ868

    Catalog No. A15937
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    JAK2 抑制剂
    CHZ868是一种有效的选择性II型JAK抑制剂,在JAK抑制剂持续性细胞,鼠类MPN模型和MPN患者样品中显示出活性。 了解更多
  19. SB1317 (TG02)

    Catalog No. A13454
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    CDK/JAK2/FLT3 抑制剂
    SB1317是细胞周期蛋白依赖性激酶(CDKs)、类FMS酪氨酸激酶-3(FLT3)和Janus激酶2(JAK2)的有效抑制剂,CDK2、JAK2和FLT3的IC50值分别为13nM、56nM和73nM。 了解更多
  20. FM-381

    Catalog No. A16805
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    JAK3 抑制剂
    FM-381是一种JAK3特异性可逆共价抑制剂,对JAK3的IC50为127 pM,相对于JAK1,JAK2和TYK2分别具有400、2、700和3,600倍的选择性。 了解更多
  21. Tyk2-IN-3

    Catalog No. A21982
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    Tyk2 pseudokinase inhibitor
    Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM. 了解更多
  22. BMS-066

    Catalog No. A21972
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    IKKβ/Tyk2 pseudokinase inhibitor
    BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. 了解更多
  23. Momelotinib Mesylate

    Catalog No. A21658
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    JAK1/JAK2 inhibitor
    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. 了解更多
  24. PF-06700841 P-Tosylate

    Catalog No. A21652
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    dual JAK1/TYK2 inhibitor
    PF-06700841 P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. 了解更多
  25. Tyk2-IN-7

    Catalog No. A21491
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    TYK2 JH2 inhibitor
    Tyk2-IN-7 (Compound 48) is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. 了解更多
  26. NVP-BSK805 dihydrochloride

    Catalog No. A21406
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    JAK2 inhibitor
    NVP-BSK805 dihydrochloride (BSK805 dihydrochloride) is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. 了解更多
  27. JAK-IN-1

    Catalog No. A21237
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    JAK1/2/3 inhibitor
    JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1. 了解更多
  28. 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
  29. 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
  30. 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
  31. 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
  32. 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
  33. 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
  34. 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
  35. 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
  36. 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
  37. 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
  38. 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
  39. XL019

    Catalog No. A12394
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    JAK2 抑制剂
    XL019是janus相关激酶2 (JAK-2)的生物可利用抑制剂,具有潜在的抗肿瘤活性。 了解更多
  40. CEP33779

    Catalog No. A12808
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    JAK2 抑制剂
    CEP33779是选择性JAK2抑制剂,IC50为1.8 nM。 了解更多
  41. 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
  42. Go 6976

    Catalog No. A12419
    PKC 抑制剂
    Go6976是一种有效的PKC抑制剂,对PKC(大鼠脑),PKCα和PKCβ1的IC50分别为7.9 nM,2.3 nM和6.2 nM。也是JAK2和Flt3的有效抑制剂。 了解更多
  43. BMS-911543

    Catalog No. A11241
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    JAK 抑制剂
    BMS-911543是一种有效的、选择性JAK2小分子抑制剂。 了解更多
  44. WP1066

    Catalog No. A11795
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    JAK 抑制剂
    WP1066是一种新型的JAK2抑制剂,可抑制携带JAK2 V617F突变的类人甲状腺细胞增殖并诱导其凋亡。 了解更多
  45. Baricitinib (LY3009104)

    Catalog No. A11329
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    JAK 抑制剂
    Baricitinib,也称为INCB028050或LY3009104,是一种选择性口服可生物利用的JAK1/JAK2抑制剂,对JAK1(5.9 nM)和JAK2(5.7 nM)具有纳摩尔浓度。 了解更多
  46. NVP-BSK805

    Catalog No. A11193
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    JAK 抑制剂
    NVP-BSK805是喹喔啉JAK2抑制剂对红细胞增多症的有效和选择性抑制,喹喔啉JAK2抑制剂可有效抑制小鼠和大鼠中重组人促红细胞生成素诱导的红细胞增多症和髓外红细胞生成。IC50为0.5 nM,比作用于JAK1, JAK3和TYK2选择性高20倍以上。 了解更多
  47. TG101209

    Catalog No. A11180
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    JAK2 抑制剂
    TG101209是一种新型的JAK2抑制剂,无细胞试验中IC50为6 nM,对Flt3和RET作用效果稍弱,IC50分别为25 nM和17 nM,作用于JAK2比作用于JAK3选择性高30倍左右,对JAK2V617F和MPLW515L/K突变型敏感。在多发性骨髓瘤中具有显着的体外活性,并且对CD45+骨髓瘤细胞显示出优先的细胞毒性。 了解更多
  48. AZ-960

    Catalog No. A10104
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    JAK2抑制剂
    AZ-960是一种有效的,选择性的和ATP竞争性的JAK2抑制剂,在体外抑制JAK2激酶的Ki为0.45 nM,并诱导成年T细胞白血病(ATL)细胞的生长停滞和凋亡 了解更多
  49. TG-101348 (Fedratinib, SAR302503)

    Catalog No. A11082
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    JAK2/FLT3 抑制剂
    TG-101348 (Fedratinib,SAR302503)是Janus相关激酶2的口服生物利用型,ATP竞争性和选择性抑制剂,在无细胞试验中IC50为3 nM,作用于JAK2比作用于JAK1和JAK3选择性高35和334倍,具有潜在的抗肿瘤活性。 了解更多
  50. 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

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