[CAS NO. 1173097-76-1] U0126-EtOH

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PRODUCTS SPECIFICATIONS [1173097-76-1]

Catalog

SLK-S1102

Brand

Selleck

CAS

1173097-76-1

DESCRIPTION [1173097-76-1]

Overview

MDL	MFCD22628895
Molecular Weight	426.56
Molecular Formula	C18H16N6S2.C2H6O
SMILES	N#CC(/C(C#N)=C(N)/SC1=CC=CC=C1N)=C(N)\SC2=CC=CC=C2N.CCO

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3443 mL	11.7217 mL	23.4434 mL
5 mM	0.4689 mL	2.3443 mL	4.6887 mL
10 mM	0.2344 mL	1.1722 mL	2.3443 mL
50 mM	0.0469 mL	0.2344 mL	0.4689 mL

Description

U0126-EtOH is a highly selective inhibitor of with of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits and with antiviral activity.

Features

A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.

Targets

MEK2 ^[1] (Cell-free assay)	MEK1 ^[1] (Cell-free assay)
0.06 μM	0.07 μM

In vitro

U0126-EtOH functionally antagonizes AP- 1 transcriptional activity and blocks the production of a variety of cytokines and metalloproteinases involved in the inflammatory response. U0126-EtOH inhibits T cell proliferation in response to antigenic stimulation or cross-linked anti-CD3 plus anti-CD28 Abs without effect on IL-2-induced proliferation by down-regulating IL-2 mRNA levels. A recent study shows that U0126-EtOH antagonizes resveratrol-induced apoptosis in castration-resistant human prostate cancer C4-2 cells, inhibits mitochondrial function and shifts cells to aerobic glycolysis independently of MEK.

In vivo

U0126-EtOH, as the inhibitor of intracellular Raf/MEK/ERK signaling pathway, demonstrates antiviral activity by suppressing propagation of the 2009 pandemic IV H1N1 variant and highly pathogenic avian influenza viruses (HPAIV) in vivo in the mouse lung by inhibiting. U0126-EtOH shows the potential neuroprotective effect and improving spatial learning in Morris water maze (MWM) by activating peroxisome proliferator-activated receptor gamma coactivator-1a, nuclear respiratory factor 1, and mitochondrial transcription factor A in Aβ-injected rats.

References

[1] Duncia JV, et al. Bioorg Med Chem Lett. 1998, 8(20), 2839-2844.
[2] DeSilva DR, et al. J Immunol. 1998, 160(9), 4175-4181.
[3] Freeman MR, et al. Cancer Biol Ther. 2011, 12(11), 966-977.
[4] Droebner K, et al. Antiviral Res. 2011, 92(2), 195-203.
[5] Ashabi G, et al. Behav Brain Res. 2012.
[6] Favata MF, et al. J Biol Chem. 1998, 273(29), 18623-18632.