G-963 

G-963 is an allosteric inhibitor of mitogen-activated protein kinase kinase (MEK) with a MEK1 IC₅₀ of 0.012 μM. G-963 interacts with Ser212 of MEK and exhibits potent antiproliferative activity against HCT116 colon cancer cells (EC₅₀ = 0.120 μM) and A375 melanoma cells (EC₅₀ = 0.025 μM). G-963 can be used for the research of colon cancer, melanoma^[1].

G-963 inhibits MEK1 with an IC₅₀ of 0.012 μM, inhibits proliferation of HCT116 colon cancer cells with an EC₅₀ of 0.120 μM and A375 melanoma cells with an EC₅₀ of 0.025 μM, and shows weak inhibition of cytochrome P450 enzymes 2C9, 2C19, 3A4, 2D6, and 1A2 with IC₅₀ values > 10 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

457.19

C₁₆H₁₃FIN₃O₄

1009330-74-8

O=C(C1=C(NC2=CC=C(C=C2F)I)C3=C(C=CN=C3)O1)NOCCO

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Robarge KD, et al. Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. Bioorg Med Chem Lett. 2014;24(19):4714-4723.  [Content Brief]