BIX 02189

Bezeichnung:BIX 02189

CAS-Nr1094614-85-3

Englisch Name:BIX 02189

CBNumberCB52537538

SummenformelC27H28N4O2

Molgewicht440.54

MOL-Datei1094614-85-3.mol

BIX 02189 physikalisch-chemischer Eigenschaften

Schmelzpunkt	>250°C (dec.)
Siedepunkt	653.4±55.0 °C(Predicted)
Dichte	1.230
storage temp.	-20°C Freezer, Under inert atmosphere
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
Aggregatzustand	Solid
pka	11.24±0.20(Predicted)
Farbe	Yellow

Sicherheit

HS Code

2933998090

Gefahreninformationscode (GHS)

BIX 02189 Chemische Eigenschaften,Einsatz,Produktion Methoden

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

BIX 02189 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

1094614-85-3, BIX 02189 Verwandte Suche:

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