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MEK1/2

MEK1/2, also known as MAPKK (mitogen-activated protein kinase kinase), is a kinase enzyme which phosphorylates MAPK (mitogen-activated protein kinase).

Products for  MEK1/2

  1. Cat.No. Product Name Information
  2. GC12851 10Z-Hymenialdisine Pan kinase inhibitor 10Z-Hymenialdisine  Chemical Structure
  3. GC15240 APS-2-79 APS-2-79 is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATPbiotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling. APS-2-79  Chemical Structure
  4. GN10063 Arctigenin Arctigenin  Chemical Structure
  5. GC17030 AZD6244(Selumetinib) A highly selective inhibitor of MEK1/2 AZD6244(Selumetinib)  Chemical Structure
  6. GC14643 AZD8330 MEK 1/2 inhibitor AZD8330  Chemical Structure
  7. GC33305 Balamapimod (MKI 833) Balamapimod (MKI 833) (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity. Balamapimod (MKI 833)  Chemical Structure
  8. GC17828 BI-847325 dual inhibitor of MEK and Aurora kinases BI-847325  Chemical Structure
  9. GC15693 BIX 02188 MEK5 inhibitor,potent and selective BIX 02188  Chemical Structure
  10. GC12220 BIX 02189 Selective MEK5 inhibitor BIX 02189  Chemical Structure
  11. GC35684 CHMFL-EGFR-202 CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ?10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines. CHMFL-EGFR-202  Chemical Structure
  12. GC10033 Cobimetinib A potent, orally available MEK1 inhibitor Cobimetinib  Chemical Structure
  13. GC14337 Cobimetinib (R-enantiomer) Cobimetinib (R-enantiomer)  Chemical Structure
  14. GC17426 Cobimetinib (racemate) Cobimetinib (racemate)  Chemical Structure
  15. GC35719 Cobimetinib hemifumarate Cobimetinib hemifumarate is a novel selective MEK1 inhibitor, and the IC50 value against MEK1 is 4.2 nM. Cobimetinib hemifumarate  Chemical Structure
  16. GC14247 GDC-0623 MEK1 inhibitor, potent and ATP-uncompetitive GDC-0623  Chemical Structure
  17. GC12006 GDC-0994 GDC-0994 (GDC-0994) is an orally active ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively. GDC-0994  Chemical Structure
  18. GC36199 GW284543 GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein. GW284543  Chemical Structure
  19. GC43885 Hypothemycin A resorcylic acid lactone polyketide Hypothemycin  Chemical Structure
  20. GN10023 Isorhamnetin Isorhamnetin  Chemical Structure
  21. GC17608 Lidocaine Anasthetic and class Ib antiarrhythmic agent Lidocaine  Chemical Structure
  22. GC33831 Lidocaine hydrochloride (Lignocaine hydrochloride) Lidocaine hydrochloride (Lignocaine hydrochloride) (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride (Lignocaine hydrochloride)  Chemical Structure
  23. GC64904 MAP855 MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2. MAP855  Chemical Structure
  24. GC11277 MEK inhibitor MEK inhibitor  Chemical Structure
  25. GC33388 MEK-IN-1 MEK-IN-1 is a MEK inhibitor extracted from patent WO2008076415A1. MEK-IN-1  Chemical Structure
  26. GC12843 MEK162 (ARRY-162, ARRY-438162) MEK162 (ARRY-162, ARRY-438162) (MEK162) is an oral and selective MEK1/2 inhibitor. MEK162 (ARRY-162, ARRY-438162) (MEK162) inhibits MEK with an IC50 of 12 nM. MEK162 (ARRY-162, ARRY-438162)  Chemical Structure
  27. GC64292 MS432 MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively. MS432  Chemical Structure
  28. GC15646 PD 184161 MEK1/2 inhibitor PD 184161  Chemical Structure
  29. GC17964 PD 198306 MEK1/2 inhibitor PD 198306  Chemical Structure
  30. GC17485 PD 334581 MEK1 inhibitor PD 334581  Chemical Structure
  31. GC10397 PD0325901

    A MEK inhibitor that sustains stem cell renewal

    PD0325901  Chemical Structure
  32. GC63554 PD0325901-O-C2-dioxolane PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader. PD0325901-O-C2-dioxolane  Chemical Structure
  33. GC12989 PD184352 (CI-1040) PD184352 (CI-1040) (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1. PD184352 (CI-1040)  Chemical Structure
  34. GC10110 PD318088 Allosteric MEK1/2 inhibitor, non-ATP competitive PD318088  Chemical Structure
  35. GC12819 PD98059

    PD98059 is a potent and selective MEK inhibitor with an IC50 of 2 μM.

    PD98059  Chemical Structure
  36. GC18050 Pimasertib (AS-703026) Pimasertib (AS-703026) (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor. Pimasertib (AS-703026)  Chemical Structure
  37. GC14732 PLX-4720 An orally-available inhibitor of the B-raf mutant B-RafV600E PLX-4720  Chemical Structure
  38. GC16872 Refametinib

    MEK 1/ MEK 2 inhibitor

    Refametinib  Chemical Structure
  39. GC37516 Refametinib R enantiomer Refametinib R enantiomer is a MEK inhibitor extracted from patent WO2007014011A2, compound 1022, has an EC50 of 2.0-15 nM. Refametinib R enantiomer  Chemical Structure
  40. GC37522 RGB-286638 A multi-kinase inhibitor RGB-286638  Chemical Structure
  41. GC37523 RGB-286638 free base A multi-kinase inhibitor RGB-286638 free base  Chemical Structure
  42. GC12141 RO4987655 MEK inhibitor RO4987655  Chemical Structure
  43. GC12406 RO5126766(CH5126766) RO5126766(CH5126766) (CH5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAFV600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively). RO5126766(CH5126766)  Chemical Structure
  44. GC16001 SCH772984

    A selective inhibitor of ERK1/2

    SCH772984  Chemical Structure
  45. GC14647 SCH772984 HCl

    ERK1/2 inhibitor

    SCH772984 HCl  Chemical Structure
  46. GC15044 SCH772984 TFA

    ERK1/2 inhibitor

    SCH772984 TFA  Chemical Structure
  47. GC38653 Selumetinib sulfate Selumetinib (AZD6244) is selective, non-ATP-competitive oral?MEK1/2?inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation. Selumetinib sulfate  Chemical Structure
  48. GC15359 SL-327 Selective MEK1/2 inhibitor SL-327  Chemical Structure
  49. GC10209 TAK-733 MEK allosteric site inhibitor TAK-733  Chemical Structure
  50. GC41573 Theaflavin 3,3'-digallate

    Theaflavin-3,3'-digallate (TFDG) is a major polyphenol found in black tea with diverse biological activities.

    Theaflavin 3,3'-digallate  Chemical Structure
  51. GC70053 Trametiglue

    Trametiglue is a derivative of Trametinib that binds to KSR-MEK and RAF-MEK with unprecedented potency and selectivity through a unique interface interaction.

    Trametiglue  Chemical Structure
  52. GC13508 Trametinib (GSK1120212)

    An inhibitor of MEK1 and MEK2

    Trametinib (GSK1120212)  Chemical Structure
  53. GC15260 Trametinib DMSO solvate Trametinib DMSO solvate  Chemical Structure
  54. GC30162 trans-Zeatin A cytokinin plant growth regulator trans-Zeatin  Chemical Structure
  55. GC45099 U-0126

    A MEK inhibitor

    U-0126  Chemical Structure
  56. GC15061 U0124 Inactive analog of U0126(MEK-1/2 inhibitor), used as a negative control U0124  Chemical Structure
  57. GC12807 U0126-EtOH

    U0126-EtOH-EtOH (U0126 has potent inhibition on MEK1 and MEK2 with IC50s of 72 nM and 58 nM, respectively

    U0126-EtOH  Chemical Structure
  58. GC13412 Vemurafenib (PLX4032, RG7204)

    An inhibitor of mutant V600E and wild type B-Raf

    Vemurafenib (PLX4032, RG7204)  Chemical Structure
  59. GC63264 Zapnometinib Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib  Chemical Structure

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