MEK

Catalog No.Inhibitor Name MEKMEK1MEK1/2MEK2MEK5Other
A10257Selumetinib
***
A10256PD0325901
****
A11029Trametinib
****
****
A10957U0126-EtOH
*
**
MKK6/p38 MAPK,MKK3/p38 MAPK
A10212PD184352
**
**
A10705PD98059
*
A10151BIX 02189
****
ERK5,TGFβR1
A10089Pimasertib
*
A10150BIX 02188
***
ERK5,TGFβR1
A11040TAK-733
****
A10115AZD8330
ERK phosphorylation
A11493Binimetinib
***
***
A14137SL-327
*
*
AP-1,MKK3/p38 MAPK
A11264Refametinib
**
**
A12974GDC-0623
****
A15762BI-847325
**
***
Aurora B,Aurora C,Aurora A
A11441Cobimetinib
***
A10704PD318088
A10453Honokiol
Akt-phosphorylation
A11247RO4927350
A13272RO4987655
****
A14019RO5126766 (CH5126766)
*
BRAF, CRAF

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.

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  1. RO4987655

    Catalog No. A13272
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    MEK1 抑制剂
    RO4987655是一种口服活性小分子,靶向有丝分裂原激活的蛋白激酶激酶1(MAP2K1或MEK1),抑制 MEK1/MEK2,IC50 为 5.2 nM。具有潜在的抗肿瘤活性。 了解更多
  2. PD184352 (CI-1040)

    Catalog No. A10212
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    MEK1/2 抑制剂
    PD184352 (CI-1040)是一种ATP非竞争性MEK1/2抑制剂,在基于细胞的测定中,IC50为17 nM,对MEK1/2的选择性是对MEK5的100倍。 了解更多
  3. AS703026 (Pimasertib)

    Catalog No. A10089
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    MEK1/2 抑制剂
    AS703026 (Pimasertib)是一种新型的,选择性的,口服可生物利用的MEK1/2抑制剂,可抑制MM细胞的生长和存活以及细胞因子诱导的破骨细胞分化。 了解更多
  4. RO5126766 (CH5126766)

    Catalog No. A14019
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    Raf/MEK dual 抑制剂
    RO5126766 (CH5126766)是对Raf和MEK丝裂原激活的蛋白激酶(MAPK)具有特异性的蛋白激酶抑制剂,具有潜在的抗肿瘤活性。 了解更多
  5. Balamapimod (MKI-833)

    Catalog No. A13119
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    Ras/Raf/MEK 抑制剂
    Balamapimod (MKI-833)是Ras/Raf/MEK抑制剂。 了解更多
  6. TAK-733

    Catalog No. A11040
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    MEK 抑制剂
    TAK-733是一种有效的,选择性的MEK变构抑制剂,作用于MEK1,IC50为3.2 nM,抑制Abl1,AKT3,c-RAF,CamK1,CDK2及c-Met等活性。 了解更多
  7. AZD8330

    Catalog No. A10115
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    MEK 抑制剂
    AZD8330是新型,选择性,非ATP竞争性MEK 1/2抑制剂,IC50为7 nM。阶段1。 了解更多
  8. PD318088

    Catalog No. A10704
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    MEK 抑制剂
    PD318088是MEK1和MEK2的抑制剂。 了解更多
  9. BIX02188

    Catalog No. A10150
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    MEK5 抑制剂
    BIX02188是一种有效的选择性MEK5抑制剂。 了解更多
  10. RO4927350

    Catalog No. A11247
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    MEK1/2 抑制剂
    RO4927350是一种有效且高度选择性的非ATP竞争性MEK1/2抑制剂。 了解更多
  11. Cobimetinib (R-enantiomer)

    Catalog No. A15051
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    MEK 抑制剂
    Cobimetinib R-enantiomer是Cobimetinib的R对映异构体,Cobimetinib是一种有力的,高选择性的促分裂原活化蛋白激酶(MEK1/2)抑制剂。 了解更多
  12. MEK inhibitor

    Catalog No. A15157
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    MEK 抑制剂
    MEK inhibitor是一种有效的MEK抑制剂,抗肿瘤剂。 了解更多
  13. BI-847325

    Catalog No. A15762
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    MEK/Aurora 抑制剂
    BI-847325是一种生物利用型选择性MEK/Aurora双重激酶抑制剂,对于非洲爪蟾Aurora B,人Aurora A和Aurora C以及IC50分别为3 nM,25 nM,15 nM,25 nM和4 nM IC50人MEK1和MEK2。 了解更多
  14. G-479

    Catalog No. A14380
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    MEK 抑制剂
    G-479是有效的MEK抑制剂。在许多方面,极性分布在整个分子中的G-479被证明具有比GDC-0623更高的生物活性。 了解更多
  15. GDC-0623

    Catalog No. A12974
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    MEK1 抑制剂
    GDC-0623是一种有效的ATP竞争性MEK1抑制剂,Ki为0.13 nM。 了解更多
  16. PD 198306

    Catalog No. A16032
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    MEK 抑制剂
    PD 198306是一种有效的,选择性的和非ATP竞争性MAPK/ERK激酶(MEK)抑制剂。 了解更多
  17. PD 334581

    Catalog No. A16044
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    MEK1 抑制剂
    PD 334581在生物学研究中用于评估卤素键合,作为合理药物设计的新型相互作用。它也是MEK1的抑制剂。 了解更多
  18. GW284543

    Catalog No. A18808
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    MEK5 inhibitor
    GW284543, also known as UNC10225170;, is a potent and selective MEK5 inhibitor with the potential for cancer treatment. 了解更多
  19. EBI-1051

    Catalog No. A13176
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    MEK inhibitor
    EBI-1051 is a highly potent and orally efficacious MEK inhibitor with an IC50 of 3.9 nM. 了解更多
  20. Cobimetinib hemifumarate

    Catalog No. A18033
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    MEK1 inhibitor
    Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM. 了解更多
  21. Trametinib (DMSO solvate)

    Catalog No. A21450
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    MEK inhibitor
    Trametinib DMSO solvate (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is a potent MEK inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM. 了解更多
  22. BIX02189

    Catalog No. A21729
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    MEK5 inhibitor
    BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM. 了解更多
  23. Cobimetinib (racemate)

    Catalog No. A15050
    MEK 抑制剂
    Cobimetinib (racemate)是一种有效的,高度选择性的MEK1/2抑制剂。 了解更多
  24. Refametinib

    Catalog No. A11264
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    MEK 抑制剂
    Refametinib是一种有效的,ATP非竞争性和高度选择性的MEK1和MEK2抑制剂,IC50分别为19 nM和47 nM。 了解更多
  25. SL-327

    Catalog No. A14137
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    MKK/MEK 抑制剂
    SL-327是MEK1和MEK2的选择性抑制剂(IC50值分别为0.18和0.22μM);在体外阻断海马LTP。全身性给药后,体内的脑渗透剂会阻止大鼠的恐惧条件和学习,并在小鼠中产生神经保护作用。 了解更多
  26. Refametinib (RDEA-119, BAY 86-9766)

    Catalog No. A12866
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    MEK1/2 抑制剂
    Refametinib (RDEA-119,BAY 86-9766)是一种口服生物利用型选择性MEK抑制剂,EC50为 2.0-15 nM。具有潜在的抗肿瘤活性。 了解更多
  27. MEK162 (ARRY-438162, Binimetinib)

    Catalog No. A11493
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    MEK1/2 抑制剂
    MEK162 (ARRY-438162,Binimetinib)是MEK1/2的一种强效、选择性ATP非竞争性抑制剂。 了解更多
  28. GDC-0973 (Cobimetinib)

    Catalog No. A11441
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    MEK1 抑制剂
    GDC-0973 (Cobimetinib,RG7420)是一种有效且高度选择性的MEK1抑制剂,IC50为4.2 nM,对MEK1的选择性选择性是对MEK2的100倍以上,并且当针对一组超过100个丝氨酸的抑制剂进行测试时,没有显示出明显的抑制作用。 了解更多
  29. BIX 02189

    Catalog No. A10151
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    MEK 抑制剂
    BIX 02189是选择性双重MEK5和ERK5(或BMK1)激酶抑制剂,对于MEK5,ERK5,TGFbR1和其他紧密相关的激酶,IC50值分别为1.5、59、580和> 6200 nM。 了解更多
  30. GSK1120212 (JTP-74057, Trametinib)

    Catalog No. A11029
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    MEK 抑制剂
    GSK1120212 (JTP-74057,Trametinib)强烈阻止了MEK1和MEK2激酶的活性,而不是其他98种激酶的活性。 了解更多
  31. U0126-EtOH

    Catalog No. A10957
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    MEK 抑制剂
    U0126-EtOH是MEK1和MEK2的抑制剂,IC50分别为72 nM和58 nM。 了解更多
  32. PD98059

    Catalog No. A10705
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    MEK 抑制剂
    PD98059是一种非ATP竞争性的MEK抑制剂,无细胞试验中IC50为2 μM,特异性抑制MEK-1介导的MAPK激活;不直接抑制ERK1或ERK2。 了解更多
  33. AZD6244 (Selumetinib)

    Catalog No. A10257
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    MEK 抑制剂
    Selumetinib (AZD6244)是一种有效,高选择性的MEK抑制剂,ARRY142886,AZD-6244和ARRY-142886是MEK 1/2抑制剂,GI50值在14至50 nm之间。 了解更多
  34. PD0325901

    Catalog No. A10256
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    MEK 抑制剂
    PD0325901是一种选择性的,非ATP竞争性MEK抑制剂,无细胞试验中IC50为0.33 nM,对ERK1和ERK2磷酸化抑制作用比CI-1040强500倍左右。 了解更多

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