ERK1/2 inhibitor 1 Chemical Properties

Density 

1.344±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 250 mg/mL (454.50 mM; Need ultrasonic)

pka

13.73±0.46(Predicted)

form 

Solid

color 

Off-white to light yellow

ERK1/2 inhibitor 1 Usage And Synthesis

Uses

ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively[1].

Biological Activity

ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively[1]. ERK1/2 inhibitor 1 (Compound 27) shows excellent antiproliferative potency with IC50s of 4.9 and 7.5 nM in A375 and Colo205 cells, respectively[1].

IC 50

ERK2: 3.0 nM (IC₅₀); ERK1

References

[1]. Heightman TD, et al. Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2. J Med Chem. 2018 Jun 14;61(11):4978-4992.