For R&D use only.

BIX02188

  • Catalog NO.:A2158
  • CAS No. : 1094614-84-2
  • Molecular Formula:C25H24N4O2
  • Molecular Weight: 412.48
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Product Details

CAS Number 1094614-84-2 Appearance
Catalog Number A2158 MDL Number MFCD14584538
Molecular Formula C25H24N4O2 Molecular Weight 412.48
Boiling Point 615.8±55.0°C at 760 mmHg Melting Point
Flash Point Density
Synonyms 3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indole-6-carboxamide;(Z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxamide;BIX-02188(Random Configuration)
Storage Condition Store in a tightly closed container,in a cool and dry place

Safety

GHS Pictogram
Signal Word Warning UN Number
Hazard Statements H302-H315-H319-H335 Class
Precautionary Statements P261-P305+P351+P338 Packing Group

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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BIX02188
3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indole-6-carboxamide;(Z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxamide;BIX-02188(Random Configuration)