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U-0126

MEK inhibitor



BML-EI282-0001	1 mg	87.00 USD

BML-EI282-0005	5 mg	336.00 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 Details

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 Temperature

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

Regulatory Status:	RUO - Research Use Only

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Product Literature References

Picolinafen exposure induces ROS accumulation and calcium depletion, leading to apoptosis in porcine embryonic trophectoderm and uterine luminal epithelial cells: W. Park, et al.; Theriogenology 201, 12 (2023), Abstract;

Aclonifen induces bovine mammary gland epithelial cell death by disrupting calcium homeostasis and inducing ROS production: J. Park, et al.; Pestic. Biochem. Physiol. 181, 105011 (2022), Abstract;

Chemosynthetic ethanolamine plasmalogen stimulates gonadotropin secretion from bovine gonadotrophs by acting as a potential GPR61 agonist: H. Kadokawa, et al.; Anim. Reprod. Sci. 241, 106992 (2022), Abstract;

Hesperidin Suppresses the Proliferation of Prostate Cancer Cells by Inducing Oxidative Stress and Disrupting Ca2+ Homeostasis: S.A. Jeong, et al.; Antioxidants 11, 1633 (2022), Abstract;

Diflubenzuron leads to apoptotic cell death through ROS generation and mitochondrial dysfunction in bovine mammary epithelial cells: W. Lee, et al.; Pestic. Biochem. Physiol. 177, 104893 (2021), Abstract;

Exposure to fipronil induces cell cycle arrest, DNA damage, and apoptosis in porcine trophectoderm and endometrial epithelium, leading to implantation defects during early pregnancy: W. Park, et al.; Environ. Pollut. 291, 118234 (2021), Abstract;

Fluroxypyr-1-methylheptyl ester causes apoptosis of bovine mammary gland epithelial cells by regulating PI3K and MAPK signaling pathways and endoplasmic reticulum stress: G. Am, et al.; Pestic. Biochem. Physiol. 180, 105003 (2021), Abstract;

Nemo-like kinase drives Foxp3 stability and is critical for maintenance of immune tolerance by regulatory T cells: V. Fleskens, et al.; Cell Rep. 26, 3600 (2019), Abstract; Full Text

Carbon monoxide releasing molecule-2 attenuates Pseudomonas aeruginosa-induced ROS-dependent ICAM-1 expression in human pulmonary alveolar epithelial cells: C.W. Lee, et al.; Redox Biol. 18, 93 (2018), Abstract; Full Text

CCL4 enhances preosteoclast migration and its receptor CCR5 downregulation by RANKL promotes osteoclastogenesis: D. Lee, et al.; Cell Death Dis. 9, 495 (2018), Abstract; Full Text

Chrysin attenuates progression of ovarian cancer cells by regulating signaling cascades and mitochondrial dysfunction: W. Lim, et al.; J. Cell. Physiol. 233, 3129 (2018), Abstract;

Fibroblast growth factor 2 induces proliferation and distribution of G2 /M phase of bovine endometrial cells involving activation of PI3K/AKT and MAPK cell signaling and prevention of effects of ER stress: W. Lim, et al.; J. Cell. Physiol. 233, 3295 (2018), Abstract;

Sideroxylin (Callistemon lanceolatus) suppressed cell proliferation and increased apoptosis in ovarian cancer cells accompanied by mitochondrialdysfunction, the generation of reactive oxygen species, and an increase of lipid peroxidation: S. Park, et al.; J. Cell. Physiol. 233, 8597 (2018), Application(s): Treatment of ovarian cancer cells (ES2 and OV90), Abstract;

The O-methylated isoflavone, formononetin, inhibits human ovarian cancer cell proliferation by sub G0/G1 cell phase arrest through PI3K/AKT and ERK1/2 inactivation: S. Park, et al.; J. Cell. Biochem. 119, 7377 (2018), Application(s): Treatment of ovarian cancer cells (ES2 and OV90), Abstract;

Tributyltin Inhibits Neural Induction of Human Induced Pluripotent Stem Cells: S. Yamada, et al.; Sci. Rep. 8, 12155 (2018), Abstract; Full Text

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;