BIX 02189 Chemical Structure
AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM.
CI-1040 (PD184352) is a MEK 1/2 inhibitor. Ki of 300nM
PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.
MEK inhibitor with EC50 of 73 nM.
U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.
PD 98059 is an inhibitor of MEK1 and MEK2 with IC50 values of 4 μM and 50 μM respectively.
AS703026 is a highly selective and potent noncompetitive inhibitor of MEK1/2 with an IC50 range of 5-11 nM.
BIX02188 is a MEK5-selective inhibitor with an IC50 of 0.8 ± 1.0 μM.
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor.
AZD8330 is an orally active, selective MEK inhibitor with an IC50 of 7 nM.
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]
| 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 |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
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A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules

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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