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Home >> Signaling Pathways >> MAPK Signaling >> MEK1/2

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. GC73085 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles 3-droxy-4-carboxyalkylamidino-5-arylamino-isothiazoles is an inhibitor for bone morphogenetic protein 2 (BMP2) with an IC50 of 2.2 μM. 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles Chemical Structure
  4. 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
  5. GN10063 Arctigenin Arctigenin,a natural lignan compound,has demonstrated anticancer activities in cancer. Arctigenin exhibits potent antioxidant, anti-inflammatory and antiviral (influenza A virus) activities. Arctigenin Chemical Structure
  6. GC17030 AZD6244(Selumetinib)

    AZD6244; ARRY-142886

     A highly selective inhibitor of MEK1/2 AZD6244(Selumetinib) Chemical Structure
  7. GC14643 AZD8330

    ARRY-424704; ARRY-704; AZD-8330; ARRY424704; ARRY704; AZD8330

     MEK 1/2 inhibitor AZD8330 Chemical Structure
  8. GC33305 Balamapimod (MKI 833)

    MKI 833

     Balamapimod (MKI 833) (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity. Balamapimod (MKI 833) Chemical Structure
  9. GC17828 BI-847325 dual inhibitor of MEK and Aurora kinases BI-847325 Chemical Structure
  10. GC15693 BIX 02188 MEK5 inhibitor,potent and selective BIX 02188 Chemical Structure
  11. GC12220 BIX 02189 Selective MEK5 inhibitor BIX 02189 Chemical Structure
  12. 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
  13. GC10033 Cobimetinib

    GDC-0973, RG-7420, XL518

     A potent, orally available MEK1 inhibitor Cobimetinib Chemical Structure
  14. GC14337 Cobimetinib (R-enantiomer) Cobimetinib (R-enantiomer) Chemical Structure
  15. GC17426 Cobimetinib (racemate) Cobimetinib (racemate) Chemical Structure
  16. 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
  17. GC14247 GDC-0623

    RG 7421; MEK inhibitor 1

     MEK1 inhibitor, potent and ATP-uncompetitive GDC-0623 Chemical Structure
  18. GC12006 GDC-0994

    Ravoxertinib

     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
  19. GC69191 GSK1790627

    GSK1790627 is the N-deacetylated metabolite of Trametinib. Trametinib is an orally active MEK inhibitor that activates autophagy and induces cell apoptosis.

     GSK1790627 Chemical Structure
  20. GC36199 GW284543

    UNC10225170

     GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein. GW284543 Chemical Structure
  21. GC43885 Hypothemycin

    NSC 354462

     A resorcylic acid lactone polyketide Hypothemycin Chemical Structure
  22. GN10023 Isorhamnetin

    3'Omethyl Quercetin

     Isorhamnetin Chemical Structure
  23. GC17608 Lidocaine

    NSC 40030

     Anasthetic and class Ib antiarrhythmic agent Lidocaine Chemical Structure
  24. 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
  25. 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
  26. GC11277 MEK inhibitor MEK inhibitor Chemical Structure
  27. GC33388 MEK-IN-1 MEK-IN-1 is a MEK inhibitor extracted from patent WO2008076415A1. MEK-IN-1 Chemical Structure
  28. GC73446 MEK-IN-6 MEK-IN-6 (Example 69) is a MEK inhibitor. MEK-IN-6 Chemical Structure
  29. GC12843 MEK162 (ARRY-162, ARRY-438162)

    ARRY-438162, MEK162

     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
  30. 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
  31. GC73498 MS934 MS934 is a novel improved VHL-recruiting MEK 1/2 degrader. MS934 Chemical Structure
  32. GC91576 Nedometinib

    NFX-179

     Nedometinib is a MEK1 inhibitor (IC50 = 135 nM). Nedometinib Chemical Structure
  33. GC73789 NST-628 NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 Chemical Structure
  34. GC15646 PD 184161 MEK1/2 inhibitor PD 184161 Chemical Structure
  35. GC17964 PD 198306 MEK1/2 inhibitor PD 198306 Chemical Structure
  36. GC17485 PD 334581 MEK1 inhibitor PD 334581 Chemical Structure
  37. GC10397 PD0325901 PD0325901 is an orally active, selective and non-ATP-competitive mitogen-activated protein kinase kinase (MEK) inhibitor with an IC50 value of 0.33nM. PD0325901 Chemical Structure
  38. 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
  39. GC12989 PD184352 (CI-1040)

    PD 184352

     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
  40. GC10110 PD318088 Allosteric MEK1/2 inhibitor, non-ATP competitive PD318088 Chemical Structure
  41. GC12819 PD98059

    NSC 679828

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

     PD98059 Chemical Structure
  42. GC18050 Pimasertib (AS-703026)

    MSC1936369B, Pimasertib

     Pimasertib (AS-703026) (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor. Pimasertib (AS-703026) Chemical Structure
  43. GC14732 PLX-4720

    Raf Kinase Inhibitor V

     An orally-available inhibitor of the B-raf mutant B-RafV600E PLX-4720 Chemical Structure
  44. GC16872 Refametinib

    BAY 869766; RDEA119;

    MEK 1/ MEK 2 inhibitor

     Refametinib Chemical Structure
  45. 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
  46. GC37522 RGB-286638 A multi-kinase inhibitor RGB-286638 Chemical Structure
  47. GC37523 RGB-286638 free base A multi-kinase inhibitor RGB-286638 free base Chemical Structure
  48. GC12141 RO4987655

    CH4987655

     MEK inhibitor RO4987655 Chemical Structure
  49. GC12406 RO5126766(CH5126766)

    CH5126766, VS-6766

     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
  50. GC16001 SCH772984 SCH772984 is a novel, potent, ATP-competitive inhibitor of ERK1 and ERK2 with IC50 values of 4nM and 1nM, respectively. SCH772984 Chemical Structure
  51. GC14647 SCH772984 HCl

    ERK1/2 inhibitor

     SCH772984 HCl Chemical Structure
  52. GC15044 SCH772984 TFA

    ERK1/2 inhibitor

     SCH772984 TFA Chemical Structure
  53. 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
  54. GC15359 SL-327 Selective MEK1/2 inhibitor SL-327 Chemical Structure
  55. GC10209 TAK-733 MEK allosteric site inhibitor TAK-733 Chemical Structure
  56. GC41573 Theaflavin 3,3'-digallate

    TF3, TFDG

     Theaflavin 3,3'-digallate (TF-3; ZP10) is a potent inhibitor of Zika virus (ZIKV) protease with an IC50 value of 2.3μM. Theaflavin 3,3'-digallate Chemical Structure
  57. 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
  58. GC13508 Trametinib (GSK1120212)

    GSK1120212, JTP-74057

     Trametinib (GSK1120212, JTP-74057) is a second-generation small molecule inhibitor of MEK kinase. Trametinib (GSK1120212) Chemical Structure
  59. GC15260 Trametinib DMSO solvate Trametinib DMSO solvate Chemical Structure
  60. GC45902 Trametinib-13C-d3

    GSK1120212-13C,d3; JTP-74057-13C,d3

     A neuropeptide with diverse biological activities Trametinib-13C-d3 Chemical Structure
  61. GC30162 trans-Zeatin A cytokinin plant growth regulator trans-Zeatin Chemical Structure
  62. GC45099 U-0126

    A MEK inhibitor

     U-0126 Chemical Structure
  63. GC15061 U0124 Inactive analog of U0126(MEK-1/2 inhibitor), used as a negative control U0124 Chemical Structure
  64. GC12807 U0126-EtOH U0126-EtOH-EtOH (U0126), as a non-ATP competitive and selective inhibitor, a has potent inhibition on MEK1 and MEK2 with IC50s of 72 nM and 58 nM, respectively. U0126-EtOH Chemical Structure
  65. GC13412 Vemurafenib (PLX4032, RG7204)

    RG-7204, Ro 51-85426, Vemurafenib

    An inhibitor of mutant V600E and wild type B-Raf

     Vemurafenib (PLX4032, RG7204) Chemical Structure
  66. GC63264 Zapnometinib

    PD0184264; ATR-002

     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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