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HomeProduct name listBIX 02189

BIX 02189

BIX 02189 Structural

What is BIX 02189?

The Uses of BIX 02189

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

The Uses of BIX 02189

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

What are the applications of Application

BIX 02189 is a MEK5 and ERK5 catalytic activity blocker

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.

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.

Properties of BIX 02189

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 for BIX 02189

Signal word Danger
Pictogram(s)
ghs
Skull and Crossbones
Acute Toxicity
GHS06
GHS Hazard Statements H301:Acute toxicity,oral
Precautionary Statement Codes P264:Wash hands thoroughly after handling.
P264:Wash skin thouroughly after handling.
P270:Do not eat, drink or smoke when using this product.
P405:Store locked up.

Computed Descriptors for BIX 02189

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