Signaling Pathway

MEK

MEK

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Mitogen-activated protein kinase kinase (MEK, 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.

MEK Inhibitors & Modulators (26)

Product Name Catalog No. Brief Description
AS703026

HY-12042

AS703026(Pimasertib) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines.

AZD8330

HY-12058

AZD8330(ARRY-424704; ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM.

BIX02188

HY-12055

BIX02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

BIX02189

HY-12056

BIX02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.

CI-1040

HY-50295

CI-1040 is a selective MEK inhibitor (Ki = 300 nM in vitro).

Cobimetinib

HY-13064

Cobimetinib(GDC-0973; XL518) is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2).

Cobimetinib (R-enantiomer)

HY-13079

GDC-0973(XL-518) is a selective inhibitor of MEK.

Cobimetinib racemate

HY-13078

Cobimetinib(GDC-0973; XL518) is a potent, highly selective inhibitor of MEK1/2.

GDC-0623

HY-15610

GDC-0623 is a potent, ATP-uncompetitive inhibitors of MEK1(Ki=0.13 nM, +ATP); 6-fold weaker potency against HCT116 (KRAS(G13D), EC50=42 nM) versus A375 (BRAF(V600E), EC50=7 nM).

Isorhamnetin

HY-N0776

Isorhamnetin is an O-methylated flavonol, a flavonoid aglucon.

MEK inhibitor

HY-12202

MEK inhibitor is a potent MEK inhibitor, antitumor agent.

MEK162

HY-15202

MEK162(ARRY-438162; ARRY-162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM.

OTS-964

HY-12467

OTS964 is a potent TOPK inhibitor with an IC50 value of 28 nM.

PD0325901

HY-10254

PD0325901 is a selective MEK1 and MEK2 inhibitor.

PD318088

HY-12062

PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.

PD98059

HY-12028

PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2.

Refametinib

HY-14691

Refametinib (RDEA119, BAY 86-9766), is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity (IC50=19 nM MEK1; IC50=47 nM MEK2).

Refametinib R enantiomer

HY-10216

Refametinib R enantiomer (BAY 869766; RDEA119) is the only cyclopropane-1-sulfonamide derivative, and exhibits a highly selective allosteric inhibition of MEK 1/2.

Ro 5126766

HY-18652

Ro 5126766 (CH5126766) is a potent and selective dual RAF/MEK inhibitor.

RO4987655

HY-14719

RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.