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You are here:Home-Inhibitors & Agonists-Ras-Raf-MAPK-ERK Pathway-MEK (MAP2K)

Request The Product List ofMEK (MAP2K) MEK (MAP2K)

MEK (Mitogen-activated protein kinase kinase, MAPKK) is a kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). The activators of p38 (MKK3 and MKK6), JNK (MKK4 and MKK7), and ERK (MEK1 and MEK2) define independent MAP kinase signal transduction pathways. The acronym MEK derives from Mitogen/Extracellular signal-regulated Kinase. MEK is a member of the MAPK signaling cascade that is activated in melanoma. When MEK is inhibited, cell proliferation is blocked and apoptosis (controlled cell death) is induced.

Cat. No. Product Name CAS No. Information
GY04370

Vacquinol-1

5428-80-8(freebase)

Vacquinol-1 (NSC 13316) is a MKK4 (MAP2K4, MEK4) activator that induces vacuolization, induces ATP depletion in glioblastoma cells (IC50 = 3.14 uM) without affecting fibroblasts, embryonic stem cells, or osteosarcoma cells; induces rapid and specific cell death of glioma cells via membrane ruffling, cell rounding, massive macropinocytic vacuole accumulation, ATP depletion, and cytoplasmic membrane rupture; shows good brain penetrance and excellent pharmacokinetics; orally bioactive.

GY02971

APS-2-79

2002381-25-9

A small molecule compound that modulates KSR-dependent MAPK signalling by antagonizing RAF heterodimerization, and the conformational changes required for phosphorylation and activation of KSR-bound MEK (KSR2 IC50=120 nM); binds to the KSR2-MEK1 complex and impedes the assembly of RAF–KSR–MEK complexes, suppresses KSR-stimulated MEK and ERK phosphorylation and suppresses oncogenic Ras mutations; enhances the efficacy of Trametinib against cancer cell lines containing K-Ras mutations.

GY10219

MKK7-COV-3

MKK7-COV-3 (MKK7 Covalen inhibitor 3) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 5 nM, displays >1,000-fold selectivity over MKK4 (IC50=7.81 uM), shows EC50 of 1.3 uM for reduction of p-JNK in ICW assays in Beas2B cell line, without effect on p-ERK levels at 10 uM; displays remarkable selectivity against a kinome panel of 76 kinases, with very few kinases inhibited by more than 75% at 1 uM: Aurora kinase B, LRRK2, and MKK4, as well as FLT3; inhibits 60% of the CD86+ response in primary mouse B cells in response to LPS stimulation (10 μM, 2 hr pre-incubation).

GY10220

MKK7-COV-13

MKK7-COV-13 (MKK7 Covalen inhibitor 13) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 10 nM, displays >1,000-fold selectivity over MKK4 (IC50>10 uM); shows EC50 of 0.3-1.0 uM for reduction of p-JNK in HEK293 cell line, without effect on p-ERK levels at 10 uM; displays remarkable selectivity against a kinome panel of 76 kinases; inhibits the CD86+ response in primary mouse B cells in response to LPS stimulation.

GY10221

MKK7-COV-9

MKK7-COV-9 (MKK7 Covalen inhibitor 9) is a potent, selective, covalent MKK7 inhibitor, displays >1,000-fold selectivity over MKK4; displays remarkable selectivity against a kinome panel of 76 kinases; inhibits the CD86+ response in primary mouse B cells in response to LPS stimulation (EC50=4.9 uM); has half-lives >40 min in dog and rat, and significantly improved stability in human and monkey liver microsomes; MKK7-COV-9 is not cytotoxic to a panel of human cell lines.

GY10480

MMK7 inhibitor 4a

MMK7 inhibitor 4a is a potent, sepecific, covalent inhibitor of MMK7, displays >800-fold selectivity over EGFR-WT and EGFR-L858R/T790M; MMK7 inhibitor 4a formed a covalent bond to Cys218 at the end of the hinge region of MMK7; displayed an excellent selectivity profile at 1 uM against a panel of 320 kinases; potently inhibits cellular JNK at 1 uM and completely inhibited its downstream effector c-Jun with no effect on the JNK-pathway; MMK7 inhibitor 4a is a valuable probe for further investigation to elucidate the function of MKK7 in cellular studies and in vivo.

GY02331

BIX02189

1265916-41-3

BIX02189 is a potent, selective inhibitor of MEK5 catalytic activity with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity (IC50=59 nM), does not inhibits closely related kinases MEK1, MEK2, ERK2, and JNK2; ; blocks phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells, also inhibits transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade; blocks ERK5 signaling and suppresses NGF-induced neurite outgrowth in PC12 cells.

GY02209

Trametinib DMSO solvate

1187431-43-1

A potent and highly specific MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM; exhibits no inhibition on the kinase activities of c-Raf, B-Raf, ERK1/2.

GY01860

APS-2-79 hydrochloride

2002381-31-7

A small molecule compound that modulates KSR-dependent MAPK signalling by antagonizing RAF heterodimerization, and the conformational changes required for phosphorylation and activation of KSR-bound MEK (KSR2 IC50=120 nM); binds to the KSR2-MEK1 complex and impedes the assembly of RAF–KSR–MEK complexes, suppresses KSR-stimulated MEK and ERK phosphorylation and suppresses oncogenic Ras mutations; enhances the efficacy of Trametinib against cancer cell lines containing K-Ras mutations.

GY03727

Cobimetinib racemate

934662-91-6

Cobimetinib racemate is the racemate form of Cobimetinib (GDC-0973, XL518), which is a potent, highly selective inhibitor of MEK1/2.

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