Trametinib (GSK1120212; JTP74057; Trade name: Mekinist), an FDA approved anti-melanoma drug, is a novel, highly specific and orally bioactive MEK1/2 inhibitor with potential antineoplastic activity.

Selumetinib (also known as AZD6244; ARRY-142886; Koselugo) is a novel, potent, highly selective and orally bioavailable small molecule MEK1 inhibitor with anticancer activity.

Myricetin (Cannabiscetin), a naturally occuring flavonoid with antioxidant and anti tumor properties, is a novel inhibitor of MEK1 activity and transformation of JB6 P+ mouse epidermal cells.

U0126-EtOH is a novel, selective and non-ATP competitive MEK1/2 inhibitor with potential anticviral activity.

Isorhamnetin (also named as 3-Methylquercetin) is a flavonoid analog isolated from the Chinese herb Hippophae rhamnoides L.

Ro 5126766 (also known as Ro-5126766; CH5126766) is a novel, potent, first-in-class dual inhibitor of MEK/RAF mitogen-activated protein kinases (MAPKs) with anticancer activity.

RO4987655 (also known as CH-4987655) is a novel, orally bioavailable and specific small molecule inhibitor of MEK kinase with an IC50 of 5.2 nM for MEK1/MEK2.

Cobimetinib (formerly GDC0973, RG7420, XL518; trade name Cotellic) is an orally bioavailable and selective small-molecule inhibitor of MEK1 with potential anticancer activity.

TAK-733 is a novel, potent, selective and orally bioavailable allosteric (non-ATP competitive) inhibitor of MEK with potential anticancer activity.

AZD8330 (AZD-8330; ARRY-704; ARRY-424704) is an orally bioactive and non-ATP competitive (Allosteric) MEK 1/2 inhibitor with potential anticancer activity. It inhibits MEK1/2 with an IC50 of 7 nM.