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BIX02188 Chemical Structure

BIX02188

Data Sheet For research use only. Not for human use.
Cat. No. :BCP01868CAS No. :1094614-84-2Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 1094614-84-2 Cat. No. BCP01868
Name BIX02188
Synonyms BIX-02188;BIX 02188;
SMILES
Chemical Name
Formula C25H24N4O2 M. Wt 412.48
Purity 98% Storage Store at 4-8°C
Description BIX02188 shows no activity against closely related kinases MEK1, MEK2, ERK1, p38α, JNK2, TGFβR1, EGFR, and STK16 with IC50 values of 1.8 μM for TGFβR1, 3.9 μM for p38α, and >6.3 μM for other kinases. Pretreatment with BIX02188 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. BIX02188 treatment alone for 24 hours in HeLa or HEK293 cells does not show any cytotoxic effect. BIX02188 inhibits transcriptional activation of MEF2C through the MEK5/ERK5 signaling cascade in active MEK5/ERK5/MEF2C-driven luciferase expression system in HeLa and HEK293 cells with IC50 values of 1.15 μM and 0.82 μM, respectively. BIX02188 also inhibits phosphorylation of BMK1 in bovine lung microvascular endothelial cells (BLMECs) which are stimulated with 300 μM H2O2, in a dose-dependent manner, with IC50 of 0.8 μM, specifically by blocking the MEK5 signal pathway.
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