U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase (ERK) and mammalian target of rapamycin (mTOR)-p70(S6K) pathways. U0126 inhibits MEK-1 and MEK-2 with little or no effect on the activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 or Cdk4. U0126 selectively repressed anchorage-independent growth of MDA-MB231 and HBC4 cells, two lines with constitutively activated ERK. In addition, i.v. administration of U0126 (100-200 mg/kg), a specific inhibitor of MEK (MAPK/ERK kinase), protects the hippocampus against forebrain ischemia. Moreover, treatment with U0126 at 3 h after ischemia significantly reduces infarct volume after transient (3 h) focal cerebral ischemia in mice. 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.
Stem Cell Res Ther. 2019 Jan 31;10(1):48.
MagT1 regulated the odontogenic differentiation of BMMSCs induced byTGC-CM via ERK signaling pathway.
U0126 purchased from AbMole
J Immunol. 2018 Oct 1.
BMC Genomics. 2017 Sep 11;18(1):714.
The dynamic landscape of gene regulation during Bombyx mori oogenesis
U0126 purchased from AbMole
Int Immunopharmacol. 2016 Nov;40:508-516.
|Source||J Immunol (2018 Oct). Figure 3. U0126 (AbMole BioScience)|
|Incubation Time||30 min|
|Results||The addition of NF-kB- and JNK-specific inhibitors signifi-cantly attenuated the KRS-induced IL-12 production from DCs, whereas p38 kinase and ERK inhibitors only slightly affected the IL-12 production from KRS-treated DCs.|
|Source||BMC Genomics (2017). Additional file 7. U0126 (Abmole Bioscience, USA)|
|Cell Lines||pupa abdomen|
|Incubation Time||48 h|
|Results||We performed injection experiments involving several inhibitors of the insulin signaling pathway. It was observed that the development of follicles was clearly delayed and the follicles showed abnormalities (Additional file 7), and the expressions of marker genes, like Cyp18a1 and early chorion gene, were up-regulated at choriogenic stages.|
|Source||International Immunopharmacology(2016).Figure 4. U0126 (AbMole BioScience, Houston, TX)|
|Method||CD4+ T cell isolation and T cell polarization in vitro|
|Cell Lines||CD4+ T cells|
|Results||When CD4+ T cells were treated with costunolide, U0126, or SB203580, the expression of CD69 upon TCR stimulation was significantly down-regulated (Fig. 4B). Th1 and Th2 cell generation was suppressed when ERK activation was inhibited by U0126 in a similar fashion to that of costunolide, albeit the development of Th17 cells was unchanged in the presence of U0126 (Fig. 4C).|
|Cell lines||EHMES-10 cells and MSTO211H cells|
|Preparation method||Cell proliferation assay. The cell proliferation assay reagent WST-1 (4-[3-(4-lodophenyl)-2-(4-nitrophenyl)-2H-5-tetrazolio]- 1,3-benzene disulfonate) (Roche Diagnostics GmbH, Mannheim, Germany) was used to assess the effect of U0126 or LY294002 on cell growth. MPM cells (1x104 cells/well) were plated in 96-well plates (Nunc, Roskilde, Denmark) and were exposed to various concentrations of test agents dissolved in DMSO. Controls received DMSO vehicle at a concentration equal to that of drug treated cells. After drug treatment for 72 h, 10 µl of WST-1 reagent were added to each well. Absorbance was measured at 450 nm with a reference wavelength at 690 nm by an E max precision microplate reader (Molecular Devices, Tokyo, Japan).|
|Incubation time||72 h|
|Animal models||Orthotopic implantation model|
|Formulation||DMSO + PBS|
|Dosages||20, 30 and 40 mg/kg twice a week|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 30 mg/mL|
Intravenous administration of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia.
Namura S, et al. Proc Natl Acad Sci U S A. 2001 Sep 25;98(20):11569-74. PMID: 11504919.
MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.
Duncia JV, et al. Bioorg Med Chem Lett. 1998 Oct 20;8(20):2839-44. PMID: 9873633.
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LY2801653 is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).
Refametinib (BAY 86-9766, RDEA119) is a potent, highly selective and ATP non-competitive inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.
GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase (MEK1/2).
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