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BIX 02189

Catalog No.S1531 1 Review(s)
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BIX 02189 Chemical Structure

  • AZD6244 (Selumetinib)

    AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM.

  • CI-1040 (PD184352)

    CI-1040 (PD184352) is a MEK 1/2 inhibitor. Ki of 300nM

  • PD0325901

    PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.

  • RDEA119 (BAY 869766)

    MEK inhibitor with EC50 of 73 nM.

  • U0126-EtOH

    U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.

  • PD98059

    PD 98059 is an inhibitor of MEK1 and MEK2 with IC50 values of 4 μM and 50 μM respectively.

  • AS703026

    AS703026 is a highly selective and potent noncompetitive inhibitor of MEK1/2 with an IC50 range of 5-11 nM.

  • BIX 02188

    BIX02188 is a MEK5-selective inhibitor with an IC50 of 0.8 ± 1.0 μM.

  • PD318088

    PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor.

  • AZD8330

    AZD8330 is an orally active, selective MEK inhibitor with an IC50 of 7 nM.

Biological Activity

BIX 02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM. [1] It inhibited catalytic function of purified, MEK5 enzyme. The MEK5 inhibitors blocked phosphorylation of ERK5, without affecting phosphorylation of ERK1/2 in sorbitol-stimulated HeLa cells. The compounds also inhibited transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade, in a cellular trans-reporter assay system. [2]

References on BIX 02189
  • [1] Biochemical and Biophysical Research Communications 2008;377:120–125
  • [2] JOURNAL OF BIOLOGICAL CHEMISTRY August 28, 2009;284:23564–23573
Molecular Weight (WM): 440.54
Formula:

C27H28N4O2

CAS No.: 1094614-85-3
Synonyms:
N/A
Dissolve in (25°C): DMSO ≥88mg/mL 
Water <1mg/mL 
Ethanol ≥88mg/mL 
Storage: 2 years-20°CPowder
1 week-4°Cin DMSO
1 month-80°in DMSO

Quality Control & MSDS

View current batch:
COA H-NMR HPLC

Research Area

MAPK >> MEK >> MEK Inhibitors
Notes:

Related Inhibitors

Recommended Screening Libraries

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    T47D cells were pretreated 30 minutes BIX 02189(0,10,20,30,50 μM) and then co-incubated with Heregulin + BIX 02189 for 15 minutes.

  • T47D cells were pretreated 30 minutes BIX 02189(0,10,20,30,50 μM) and then co-incubated with Heregulin + BIX 02189 for 15 minutes.

  • Data independently produced by Dr Franco Izzo of Institute of Biology and Experimental Medicine---BIX 02189 purchased from Selleck
    BIX 02189 purchased from Selleck

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T47D cells were pretreated 30 minutes BIX 02189(0,10,20,30,50 μM) and then co-incubated with Heregulin + BIX 02189 for 15 minutes.

Data independently produced by Dr Franco Izzo of Institute of Biology and Experimental Medicine---BIX 02189 purchased from Selleck

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