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| | BIX 02189 Basic information |
| Product Name: | BIX 02189 | | Synonyms: | BIX 02189;(3Z)-3-[({3-[(Dimethylamino)methyl]phenyl}amino)(phenyl)methylene]-N,N-dimethyl-2-oxo-6-indolinecarboxamide;bix 2189;CS-1936;CS-39;3-(((3-((Dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide;3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide;(Z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide | | CAS: | 1094614-85-3 | | MF: | C27H28N4O2 | | MW: | 440.54 | | EINECS: | | | Product Categories: | Inhibitors;MAPK | | Mol File: | 1094614-85-3.mol |  |
| | 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 |
| | BIX 02189 Usage And Synthesis |
| Uses | BIX02189 MEK inhibitor, prevents cell proliferation and induces apoptosis. Can be applied towards treatments of cancers and proliferative cell diseases. | | Uses | BIX 02189 inhibits TGF-β1-induced lung cancer cell metastasis by directly targeting TGF-β type I receptor. | | 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. |
| | BIX 02189 Preparation Products And Raw materials |
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