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.

31 Item(s)

per page

Set Descending Direction
  1. Honokiol

    Catalog No. A10453
    Quick View
    Antiangiogenic and Antitumor Agent
    Honokiol is a lignan present in the cones, bark, and leaves of Magnolia grandiflora that has shown pro-apoptotic effects in melanoma, sarcoma, myeloma, leukemia, bladder, lung, prostate, oral squamous cell carcinoma and colon cancer cell lines. Learn More
  2. PD 334581

    Catalog No. A16044
    Quick View
    MEK1 inhibitor
    PD 334581 is used in biological studies to evaluate halogen bonding as a novel interaction for rational drug design. It is also an inhibitor of MEK1. Learn More
  3. PD 198306

    Catalog No. A16032
    Quick View
    MEK inhibitor
    PD 198306 is a potent, selective and non-ATP competitive MAPK/ERK-kinase (MEK) inhibitor. Learn More
  4. GDC-0623

    Catalog No. A12974
    Quick View
    MEK1 inhibitor
    GDC-0623 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1. Learn More
  5. G-479

    Catalog No. A14380
    Quick View
    MEK inhibitor
    G-479 is an potent MEK inhibitor. G-479 with polarity distributed throughout the molecule was shown improved bioactivity over GDC-0623 in many aspects. Learn More
  6. BI-847325

    Catalog No. A15762
    Quick View
    MEK/Aurora Inhibitor
    BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1. Learn More
  7. MEK inhibitor

    Catalog No. A15157
    Quick View
    MEK inhibitor
    MEK inhibitor is a potent MEK inhibitor, antitumor agent. Learn More
  8. Cobimetinib (R-enantiomer)

    Catalog No. A15051
    Quick View
    MEK inhibitor
    Cobimetinib R-enantiomer is the R-enantiomer of Cobimetinib, which is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2). Learn More
  9. Cobimetinib (racemate)

    Catalog No. A15050
    MEK inhibitor
    Cobimetinib is a potent, highly selective inhibitor of MEK1/2. Learn More
  10. Refametinib

    Catalog No. A11264
    Quick View
    MEK inhibitor
    Refametinib is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively. Learn More
  11. SL-327

    Catalog No. A14137
    Quick View
    MKK/MEK inhibitor
    SL-327 is a selective inhibitor of MEK1 and MEK2 (IC50 values are 0.18 and 0.22 μM respectively); blocks hippocampal LTP in vitro. Brain penetrant in vivo, blocking fear conditioning and learning in rats, and producing neuroprotection in mice, following systemic administration. Learn More
  12. BIX02188

    Catalog No. A10150
    Quick View
    MEK5 inhibitor
    BIX02188 is a potent and selective inhibitor of MEK5. Learn More
  13. GDC-0973 (Cobimetinib)

    Catalog No. A11441
    Quick View
    MEK1 inhibitor
    Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Learn More
  14. MEK162 (ARRY-438162, Binimetinib)

    Catalog No. A11493
    Quick View
    MEK1/2 inhibitor
    MEK162 (ARRY-438162) is a potent, selective, ATP uncompetitive inhibitor of MEK1/2. Learn More
  15. RO4927350

    Catalog No. A11247
    Quick View
    MEK1/2 inhibitor
    RO4927350 a potent and highly selective non-ATP-competitive MEK1/2 inhibitor. Learn More
  16. Refametinib (RDEA-119, BAY 86-9766)

    Catalog No. A12866
    Quick View
    MEK1/2 inhibitor
    Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity. Learn More
  17. Balamapimod (MKI-833)

    Catalog No. A13119
    Quick View
    Ras/Raf/MEK inhibitor
    Balamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor. Learn More
  18. RO5126766 (CH5126766)

    Catalog No. A14019
    Quick View
    Raf/MEK dual inhibitor
    RO5126766, also known as CH5126766, is a protein kinase inhibitor specific for the Raf and MEK mitogen-activated protein kinases (MAPKs) with potential anti-neoplastic activity. Learn More
  19. Hypothemycin

    Catalog No. A13750
    Quick View
    Hypothemycin is a resorcylic acid lactone polyketide. It was found to inhibit the proliferation of mouse and human T cells stimulated with anti-CD3 mAb + PMA and of human PBMC stimulated with anti-CD3 mAb alone. Learn More
  20. PD318088

    Catalog No. A10704
    Quick View
    MEK Inhibitor
    PD318088 is an inhibitor of MEK1 AND MEK2. Learn More
  21. AZD8330

    Catalog No. A10115
    Quick View
    MEK Inhibitor
    AZD8330 is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1. Learn More
  22. TAK-733

    Catalog No. A11040
    Quick View
    MEK Inhibitor
    TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity. Learn More
  23. PD0325901

    Catalog No. A10256
    Quick View
    MEK inhibitor
    PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2. Learn More
  24. AZD6244 (Selumetinib)

    Catalog No. A10257
    Quick View
    MEK inhibitor
    AZD6244 (Selumetinib) also known as Selumetinib, ARRY142886, AZD-6244 & ARRY-142886 is MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nm. Learn More
  25. PD98059

    Catalog No. A10705
    Quick View
    MEK Inhibitor
    PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase. Learn More
  26. PD184352 (CI-1040)

    Catalog No. A10212
    Quick View
    MEK1/2 inhibitor
    PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. Phase 2. Learn More
  27. U0126-EtOH

    Catalog No. A10957
    Quick View
    MEK inhibitor
    U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively. Learn More
  28. AS703026 (Pimasertib)

    Catalog No. A10089
    Quick View
    MEK1/2 inhibitor
    AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor that inhibits growth and survival of MM cells and cytokine-induced osteoclast differentiation. Learn More
  29. GSK1120212 (JTP-74057, Trametinib)

    Catalog No. A11029
    Quick View
    MEK Inhibitor
    GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases. Learn More
  30. BIX 02189

    Catalog No. A10151
    Quick View
    MEK inhibitor
    BIX 02189 is a selective dual MEK5 and ERK5 (or BMK1) kinase inhibitor, with IC50 values of 1.5, 59, 580 and >6200 nM for MEK5, ERK5, TGFbR1 and other closely related kinases respectively. Learn More
  31. RO4987655

    Catalog No. A13272
    Quick View
    MEK1 inhibitor
    RO4987655 is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. Learn More

31 Item(s)

per page

Set Descending Direction
Rewards