BIX-02189(Random Configuration)

  • Chemical Properties
CAS No. 1094614-85-3 Cat. No. BCP02223
Name BIX-02189(Random Configuration)
Synonyms BIX02189;BIX-02189;
Formula C27H28N4O2 M. Wt 440.54
  • Biological Activity
Description They are more potent than the effect caused by BIX02188 with IC50 values of 4.3 nM and 830 nM, respectively. BIX02189 shows inhibitory activity against CSF1R (FMS) with IC50 of 46 nM but displays no activity against related kinases MEK1, MEK2, ERK1, p38α, JNK2, EGFR, and STK16 with IC50 values of >3.7 μM. Pretreatment with BIX02189 inhibits sorbitol-induced phosphorylation of ERK5 in HeLa cells in a dose dependent manner, and displays no inhibitory activity against the phosphorylation of ERK1/2, p38, and JNK1/2 MAPKs. Treatment with only BIX02189 for 24 hours in HeLa or HEK293 cells does not show any cytotoxic effect. BIX02189 inhibits MEK5/ERK5/MEF2C-driven luciferase expression in HeLa and HEK293 cells with IC50 values of 0.53 μM and 0.26 μM, respectively. This is a more significant than the effect caused by BIX02188. BIX02189 inhibits the activation of ERK5, and suppresses C-terminus of Hsc70-interacting protein (CHIP) mediated p53 ubiquitination, leading to the reverse of the prote
Pathways MAPK Pathway 
Targets MEK/ERK 

Structure

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