BIX 02189 Chemical Properties

Melting point:

>250°C (dec.)

Boiling point:

653.4±55.0 °C(Predicted)

Density 

1.230

storage temp. 

-20°C Freezer, Under inert atmosphere

solubility 

DMSO (Slightly), Methanol (Slightly)

form 

Solid

pka

11.24±0.20(Predicted)

color 

Yellow

Safety Information

HS Code 

2933998090

BIX 02189 Usage And Synthesis

Uses

BIX 02189 inhibits TGF-β1-induced lung cancer cell metastasis by directly targeting TGF-β type I receptor.

Uses

BIX02189 MEK inhibitor, prevents cell proliferation and induces apoptosis. Can be applied towards treatments of cancers and proliferative cell diseases.

Definition

ChEBI: 3-[[3-[(dimethylamino)methyl]anilino]-phenylmethylidene]-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide is an indolecarboxamide.

Biological Activity

bix 02189 is a selective inhibitor of mek5 with ic50 value of 1.5 nm 1.bix 02189 belongs to the indolinone kinase inhibitor series. it selectively inhibited the catalytic activity of mek5 but not other closely related kinases such as mek1, mek2, erk2 and jnk2. bix 02189 also inhibited erk5 with ic50 value of 59 nm. in hela cells, treatment of bix 02189 inhibited the phosphorylation of erk5 but not erk1/2. besides that, bix 02189 prevented the transcription of the downstream substrate mef2c in hela and hek293 cells. moreover, in a three-dimensional lymphangiogenic sprouting assay, bix 02189 resulted in an inhibition of lymphangiogenic sprouting with a minimal effective concentration of 1 μm 1,2.

target

MEK5

References

1. tatake r j, o’neill m m, kennedy c a, et al. identification of pharmacological inhibitors of the mek5/erk5 pathway. biochemical and biophysical research communications, 2008, 377(1): 120-125.2. schulz m m p, reisen f, zgraggen s, et al. phenotype-based high-content chemical library screening identifies statins as inhibitors of in vivo lymphangiogenesis. proceedings of the national academy of sciences, 2012, 109(40): e2665-e2674.

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