U0126 Inhibitor CAS No. 109511-58-2

Cat. No.	Name	Size	Price
KI0021	U0126	1 mg	$110
	U0126	5 mg	$198
	U0126	10 mg	$318
	U0126	20 mg	$500

Chemical Characteristic

Product Name	U0126
CAS No.	109511-58-2
Molecular Weight	380.49
Formula	C₁₈H₁₆N₆S₂
Chemical Name	2,3-Bis[amino[(2-aminophenyl)thio]methylene]butanedinitrile
Smiles	C(=C(\C(=C(\Sc1c(cccc1)N)/N)\C#N)/C#N)(/Sc1c(cccc1)N)\N
Chemical Structure

Biological activities

U0126 is a highly selective inhibitor of both MEK1 and MEK2 which are human extracellular signal-regulated kinase activator kinases. The IC50 of U0126 is 72 and 58 nM against MEK1 and MEK2, respectively. U0126 functionally antagonize AP-1(activator protein 1) transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2.^[1] U0126 is a mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase inhibitor. U0126 reverses morphology and inhibits anchorage-independent growth of K_{i-ras-transformed rat fibroblasts. U0126 suppresses activation of p70S6K, but not Akt, at concentrations at which it normalizes the transformed phenotypes.^[2] U0126 exhibits a dose-dependent inhibition of A375 cell invasion through growth factor-reduced Matrigel. At 5 µM, U0126 inhibits phosphorylation of the MEK 1/2 to a non-detectable level within 24 hours. The phosphorylation of extracellular signal-related kinase 1/2 is also dramatically suppressed by the treatment with 10 µM U0126.^[3] U0126 attenuates cisplatin-induced renal injury by decreasing inflammation and apoptosis. U0126 decreases ERK1/2 phosphorylation following cisplatin administration with significant functional and histologic protection. ^[4] U0126 dose-dependently blocks the basal phosphorylation of ERK. Renal phosphorylation of ERK is reduced, in a dose-dependent manner, in rats treated with U0126.^[5]}

Protocols

U0126 is dissolved in DMSO.^[5]

References

[1] Casciani V, et al. Opposite effect of phorbol ester PMA on PTGS2 and PGDH mRNA expression in human chorion trophoblast cells. Reprod Sci. 2008, 15(1): 40-50. [2] Fukazawa H, et al. U0126 reverses Ki-ras-mediated transformation by blocking both mitogen-activated protein kinase and p70 S6 kinase pathways. Cancer Res. 2000, 60(8): 2104-2107. [3] Ge X, et al. U0126, a mitogen-activated protein kinase kinase inhibitor, inhibits the invasion of human A375 melanoma cells. Cancer Lett. 2002, 179(2): 133-140. [4] Jo SK, et al. MEK inhibitor, U0126, attenuates cisplatin-induced renal injury by decreasing inflammation and apoptosis. Kidney Int. 2005, 67(2): 458-466. [5] Bokemeyer D, et al. In vivo identification of the mitogen-activated protein kinase cascade as a central pathogenic pathway in experimental mesangioproliferative glomerulonephritis. J Am Soc Nephrol. 2002, 13(6): 1473-1480.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com