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BIX02189

Catalog No. T21295   CAS 1265916-41-3
Synonyms: BIX 02189

BIX02189 is a potent and selective inhibitor of MEK5 and ERK5(IC50 : 1.5 nM and 59 nM).

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BIX02189 Chemical Structure
BIX02189, CAS 1265916-41-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
5 mg In stock $ 77.00
10 mg In stock $ 117.00
25 mg In stock $ 213.00
50 mg In stock $ 369.00
100 mg In stock $ 549.00
1 mL * 10 mM (in DMSO) In stock $ 88.00
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Purity: 99.17%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BIX02189 is a potent and selective inhibitor of MEK5 and ERK5(IC50 : 1.5 nM and 59 nM).
Targets&IC50 RPS6KA6 (RSK4):990 nM, ERK5:59 nM, RPS6KA3 (RSK2):2.1 μM, Kit:1.1 μM, Abl1:2.4 μM, FGFR1:1 μM, CSF1R (FMS):46 nM, JAK3:440 nM, MEK5:1.5 nM, TGFβR1:580 nM, Lck:250 nM
In vitro BIX02189, which 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[1].
Synonyms BIX 02189
Molecular Weight 440.54
Formula C27H28N4O2
CAS No. 1265916-41-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 49.4 mg/mL (112.14 mM)

TargetMolReferences and Literature

1. Tatake RJ, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5. 2. Kim M, et al. Laminar flow activation of ERK5 protein in vascular endothelium leads to atheroprotective effect via NF-E2-related factor 2 (Nrf2) activation. J Biol Chem. 2012 Nov 23;287(48):40722-31. 3. Hwang AR, et al. Fluvastatin inhibits AGE-induced cell proliferation and migration via an ERK5-dependent Nrf2 pathway in vascular smooth muscle cells. PLoS One. 2017 May 22;12(5):e0178278.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Prostate Cancer Compound Library Inhibitor Library Anti-Aging Compound Library Kinase Inhibitor Library Anti-Colorectal Cancer Compound Library HIF-1 Signaling Pathway Compound Library NO PAINS Compound Library MAPK Inhibitor Library Bioactive Compounds Library Max Anti-Ovarian Cancer Compound Library

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Keywords

BIX02189 1265916-41-3 MAPK ERK MEK Mitogen-activated protein kinase kinase inhibit MAP2K MAPKK BIX 02189 BIX-02189 Extracellular signal regulated kinases Inhibitor inhibitor

 

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