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U-0126

MEK inhibitor
 
BML-EI282-0001 1 mg 66.00 USD
 
BML-EI282-0005 5 mg 254.00 USD
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Replaces Prod. #: ALX-270-237

U-0126 (Bis[amino[(2-aminophenyl)thio]methylene]butanedinitrile) is a novel, potent and selective MEK inhibitor (MEK1; IC50=72nM, MEK2; IC50=58nM). Inhibits AP-1 transcription activity. Blocks the production of inflammatory cytokines and matrix metalloproteinases.

Product Specification

Formula:C18H16N6S2
 
MW:380.5
 
CAS:109522-58-2
 
Purity:≥98% (TLC)
 
Purity Detail:In solution, U 0126 forms a mixture of isomers, but this does not affect biological activity.
 
Appearance:White solid
 
Solubility:Soluble in DMSO (>10mg/ml) or 100% ethanol (2mg/ml).
 
Shipping:Ambient
 
Long Term Storage:Ambient
 
Use/Stability:Store, as supplied, at room temperature for up to 1 year.  Store solutions at -20°C for up to 3 months.
 
Scientific Background:Binding of extracellular growth factors to cell surface receptors often results in actiavtion of the mitogen-ativated protein kinase (MAPK).  MAPK is regulated by MAPK kinase , also called MEK. Deprivation of growth factors during cell culture or intracellular MEK inhibition leads to inhibition of proliferation and apoptotic cell death. N Blank et al. (2002) have shown that U0126, a common used MEK inhibitor and compound that itself has no intrinsic fluorescence in vitro but develops an intensive fluorsecence during cell culture which can be observed in all fluorescence channels with a predominance in the FL1 channel (525nm). Therefore either the use of PD98,059 or PD184352 as an alternative for U126 or nonfluorometric methods for detection of apoptosis should be considered.
 
Technical Info/Product Notes:Replacement for ADI-HPK-113
 
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Product Literature References

Additive effects of low concentrations of estradiol-17β and progesterone on nitric oxide production by human vascular endothelial cells through shared signaling pathways: Y. Pang & P. Thomas; J. Steroid Biochem. Mol. Biol. 165, 258 (2017), Application(s): Effects of steroids and inhibitors on NO production, Abstract;
Involvement of PI3K and PKA pathways in mouse tongue epithelial differentiation: J.K. Jung, et al.; Acta Histochem. 119, 92 (2017), Abstract;
AMPK activates LXRα and ABCA1 expression in human macrophages: M. Kemmerer, et al.; Int. J. Biochem. Cell Biol. 16, 30154 (2016), Application(s): Cell culture using human monocytic cells, Abstract;
Baicalein and U0126 suppress human breast cancer cell line MCF-7 through regulating MAPK signaling pathway : H. An, et al.; Int. J. Clin. Exp. Pathol. 9, 10266 (2016), Application(s): CCK8 assay, human breast cancer cell line MCF-7, Full Text
Delphinidin suppresses proliferation and migration of human ovarian clear cell carcinoma cells through blocking AKT and ERK1/2 MAPK signaling pathways: W. Lim, et al. ; Mol. Cell. Endocrinol. 422, 172 (2016), Application(s): Cell culture, Abstract;
Epidermal Growth Factor: Porcine Uterine Luminal Epithelial Cell Migratory Signal during the Peri-implantation Period of Pregnancy: W. Jeong, et al.; Mol. Cell. Endocrinol. 420, 66 (2016), Application(s): Porcine cell culture , Abstract;
Erianin inhibits high glucose-induced retinal angiogenesis via blocking ERK1/2-regulated HIF-1α-VEGF/VEGFR2 signaling pathway: Z. Yu, et al.; Sci. Rep. 6, 34306 (2016), Application(s): Effects on HG-induced HIF-1α and ERK1/2, choroid-retinal endothelial RF/6A cells, Abstract; Full Text
Eupafolin nanoparticles protect HaCaT keratinocytes from particulate matter-induced inflammation and oxidative stress: Z.C. Lin, et al.; Int. J. Nanomedicine 11, 3907 (2016), Application(s): Cell treatment to see effect on PM-induced phosphorylation, Abstract; Full Text
Hepatocyte-protective effect of nectandrin B, a nutmeg lignan, against oxidative stress: Role of Nrf2 activation through ERK phosphorylation and AMPK-dependent inhibition of GSK-3β: J.S. Song, et al.; Toxicol. Appl. Pharmacol. 307, 138 (2016), Application(s): Role of ERK and p38 signaling pathways in the activation of Nrf2/ARE pathway by nectandrin B, Abstract;
Naringenin-Induced Migration of Embrynoic Trophectoderm Cells is Mediated via PI3K/AKT and ERK1/2 MAPK Signaling Cascades: W. Lim, et al.; Mol. Cell. Endrocrinol. 428, 28 (2016), Application(s): Cell culture, Abstract;
TNF-α increases the expression and activity of vitamin D receptor in keratinocytes: role of c-Jun N-terminal kinase: E. Ziv, et al.; Dermatoendocrinol. 8, e1137399 (2016), Application(s): Cell culture, Abstract; Full Text
Effects of bleaching on osteoclast activity and their modulation by osteostatin and fibroblast growth factor 2: C. Torres-Rodriguez, et al.; J. Colloid Interface Sci. 461, 285 (2015), Application(s): Human cell culture, Abstract;
Involvement of JNK and Caspase Activation in Hoiamide A-Induced Neurotoxicity in Neocortical Neurons: Z. Cao, et al.; Mar. Drugs 13, 903 (2015), Application(s): Cell Culture, Abstract; Full Text
MEK1/2 inhibitors sensitize Bcr/Abl+ human leukemia cells to the dual Abl/Src inhibitor BMS-354/825: T.K. Nguyen, et al.; Blood 109, 4006 (2007), Abstract;
MEK inhibition enhances paclitaxel-induced tumor apoptosis: J.P. MacKeigan, et al.; J. Biol. Chem. 275, 38953 (2000), Abstract;
Identification of a novel inhibitor of mitogen-activated protein kinase kinase: M.F. Favata, et al.; J. Biol. Chem. 273, 18623 (1998), Abstract;
Inhibition of mitogen-activated protein kinase kinase blocks T cell proliferation but does not induce or prevent anergy: D.R. DeSilva, et al.; J. Immunol. 160, 4175 (1998), Abstract;
MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products: J.V. Duncia, et al.; Bioorg. Med. Chem. Lett. 8, 2839 (1998), Abstract;

General Literature References

MEK inhibitor U0126 interferes with immunofluorescence analysis of apoptotic cell death: N. Blank et al.; Cytometry 48, 179 (2002), Abstract;

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