BT2 is a thermostable small-molecule inhibitor of vascular permeability and angiogenesis, interacts with MEK1 and inhibits ERK phosphorylation, FosB/ΔFosB, and VCAM-1 expression.BT2 blocks endothelial FosB/ΔFosB expression, proliferation, migration and wound repair after in vitro injury and network formation.BT2 also inhibited a range of other regulatory genes involved in cell proliferation, migration, angiogenesis, and inflammation including intercellular adhesion molecule-1 (ICAM-1), CXCL2, KLF5, Egr-1, and Fos.BT2 reduced retinal leakage in rats at least as effectively as aflibercept, a first-line therapy for nAMD/DR.

BSJ-04-122 is a potent, selective, covalent dual MKK4/7 inhibitor with IC50 of 4/181 nM, displays excellent kinome selectivity; BSJ-04-122 covalently targets a conserved cysteine (Cys247 for MKK4, and Cys261 for MKK7) located before the DFG motif. SJ-04-122 exhibits potent cellular target engagement and induces robust target-specific downstream effects. In breast cancer cell lines, BSJ-04-122 potently inhibited JNK phosphorylation, BSJ-04-122 significantly decreased levels of T183/Y185 pJNK at 5 uM, resulting in complete inhibition at 10 uM in MDA-MB-231 cells. The combination of the dual MKK4/7 inhibitor BSJ-04-122 with a selective, covalent JNK inhibitor (JNK-IN-8) demonstrated an enhanced antiproliferative activity against triple-negative breast cancer cells.

(R)-STU104 is a potent, first-in-class TAK1-MKK3 porotein-protein interaction (PPI) inhibitor with SPR Kd of 71 nM for binding MKK3, disrupting the TAK1 phosphorylating MKK3.(R)-STU104 exhibited the potent inhibitory activity on TNF-α production on RAW264.7 cells with IC50 of 0.58 uM, suppressed the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways.(R)-STU104 demonstrated remarkable dose-effect relationships on both acute and chronic mouse ulcerative colitis (UC) models.(R)-STU104 showed better anti-UC efficacy in vivo at 10 mg/kg/d than mesalazine at the dose of 50 mg/kg/d.

PD-334581 is a MEK1 inhibitor.

A potent, orally-active MEK1/2 inhibitor with IC50 of 10-100 nM.

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

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.

CI-1040 (PD 184352) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM.

MEK4 inhibitor-2 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 83 nM.

MEK4 inhibitor-1 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 61 nM.

Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities.

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.

BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.