MEK

MEK, also known as Mitogen-activated protein kinase kinase and MAP2K, is a kinase enzyme that phosphorylates mitogen activated protein kinases (MAPKs), ERK, p38 and JNK. Seven MEK subtypes have been identified, all mediate cellular responses to different growth signals.

Products
Background
Literature
Pathways
Gene Data

Inhibitors

Cat No Product Name / Activity
1777 Arctigenin
Potent MEK1 inhibitor. Also inhibits IκBα phosphorylation
4842 BIX 02189
Selective MEK5 and ERK5 inhibitor
1532 10Z-Hymenialdisine
Pan kinase inhibitor; potently inhibits MEK1
4192 PD 0325901
Potent inhibitor of MEK1/2
4237 PD 184352
Selective MEK inhibitor
2605 PD 198306
Selective inhibitor of MEK1/2
4824 PD 334581
MEK1 inhibitor
1213 PD 98059
MEK inhibitor
1969 SL 327
Selective inhibitor of MEK1 and MEK2; brain penetrant
1868 U0124
Inactive analog of U0126 (Cat. No. 1144)
1144 U0126
Potent, selective inhibitor of MEK1 and 2

Ligand-sets

Cat No Product Name / Activity
2243 MEK Inhibitor Tocriset™
Selection of 3 MEK inhibitors (Cat. Nos. 1213, 1969 and 1144)

MEK, also known as Mitogen-activated protein kinase kinase and MAP2K, is a kinase enzyme that phosphorylates mitogen activated protein kinases (MAPKs), ERK, p38 and JNK. Seven MEK subtypes have so far been identified; MEK1 and MEK2 activate ERK, MEK3 and MEK4 activate p38 and MEK5 and MEK6 activate JNK. Upon activation, MAPKs can phosphorylate a variety of intracellular targets including transcription factors, transcriptional adaptor proteins, membrane and cytoplasmic substrates, and other protein kinases.

MEK is a key enzyme in the Ras/Raf/MEK/ERK signal transduction pathway and mediates cellular responses to different growth signals. This pathway is frequently deregulated in cancer, which makes these enzymes a candiate target for pharmacological antineoplastic treatment.

Literature for MEK

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
MAPK Signaling

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.

Pathways for MEK

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.

MEK Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
MEK1 Human MAP2K1 NM_002755 Q02750
Mouse Map2k1 NM_008927 P31938
Rat Map2k1 NM_031643 Q01986
MEK2 Human MAP2K2 NM_030662 P36507
Mouse Map2k2 NM_023138 Q63932
Rat Map2k2 NM_133283 P36506
MEK3 Human MAP2K3 NM_145109 P46734
Mouse Map2k3 NM_008928 O09110
Rat Map2k3 BC100095 Q498S1
MEK4 Human MAP2K4 NM_003010 P45985
Mouse Map2k4 NM_009157 P47809
Rat Map2k4 NM_001030023 Q4KSH6
MEK5 Human MAP2K5 NM_145162 Q13163
Mouse Map2k5 NM_011840 Q9WVS7
Rat Map2k5 NM_017246 Q62862
MEK6 Human MAP2K6 NM_002758 P52564
Mouse Map2k6 NM_011943 P70236
Rat Map2k6 NM_053703 Q925D6