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U0126

Catalog No. T21332   CAS 109511-58-2
Synonyms: U 0126, U-0126

U0126, an effective and selective non-competitive inhibitor of MAP kinase, inhibits MEK-1 and MEK-2 with IC50 values of 0.07 and 0.06 μM respectively. U0126 inhibits autophagy and mitophagy.

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U0126 Chemical Structure
U0126, CAS 109511-58-2
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1 mg Inquiry $ 195.00
5 mg Inquiry $ 437.00
10 mg Inquiry $ 655.00
25 mg Inquiry $ 1,178.00
50 mg Inquiry $ 1,768.00
100 mg Inquiry $ 2,652.00
200 mg Inquiry $ 3,978.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description U0126, an effective and selective non-competitive inhibitor of MAP kinase, inhibits MEK-1 and MEK-2 with IC50 values of 0.07 and 0.06 μM respectively. U0126 inhibits autophagy and mitophagy.
Targets&IC50 MEK2:60 nM (IC50), MEK1:70 nM (IC50)
In vitro Rat hepatocarcinoma cells (FAO) stimulated by fetal calf serum (FCS) exhibits a significant proportion in S phase (32.62%) whereas U0126 strongly decreases the proportion of cells in S phase (9.92%) and increases the proportion of cells in G0-G1 phase and to a lesser extent in G2/M[1]. U0126 efficiently reduces progeny virus titers of all tested strains in A549 cells. While nM concentrations of U0126 are efficient to reduce H1N1v and H5N1 (MB1), μM concentrations of U0126 are required to reduce the virus titer of H5N1 (GSB) and H7N7. The EC50 values for U0126-EtOH against H1N1v are 1.2 μM in A549 cells and 74.7 μM in MDCKII cells[2].
In vivo In mice, U0126-EtOH (U0126; i.p., 10.5 mg/kg) inhibits tumor growth with a 60-70% reduction 9 days after injection and thereafter[1]. After treatment with U0126-EtOH(U0126; i.p., 30 mg/kg), the vasoconstriction to S6c is markedly reduced in rats[3].
Synonyms U 0126, U-0126
Molecular Weight 832.97
Formula C43H48N10O6S
CAS No. 109511-58-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Soluble

H2O: Soluble

TargetMolReferences and Literature

1. Bessard A, et al. RNAi-mediated ERK2 knockdown inhibits growth of tumor cells in vitro and in vivo. Oncogene. 2008 Sep 11;27(40):5315-25. 2. Droebner K, et al. Antiviral activity of the MEK-inhibitor U0126 against pandemic H1N1v and highly pathogenic avian influenza virus in vitro and in vivo. Antiviral Res. 2011, 92(2), 195-203. 3. Ahnstedt H, et al. U0126 attenuates cerebral vasoconstriction and improves long-term neurologic outcome after stroke in female rats. J Cereb Blood Flow Metab. 2015 Mar;35(3):454-60. 4. Favata MF, et al. Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J Biol Chem. 1998 Jul 17;273(29):18623-32. 5. Du P, Hu T, An Z, et al. In vitro and in vivo synergistic efficacy of ceritinib combined with programmed cell death ligand‐1 inhibitor in anaplastic lymphoma kinase‐rearranged non‐small‐cell lung cancer[J]. Cancer Science. 2020, 111(6): 1887.

TargetMolCitations

1. Li W Y, Shi T S, Huang J, et al.Activation of the mTORC1 signaling cascade in the hippocampus and medial prefrontal cortex is required for the antidepressant actions of vortioxetine in mice.International Journal of Neuropsychopharmacology.2023: pyad017. 2. Shen S, Huang Z, Lin L, et al.Tussilagone attenuates atherosclerosis through inhibiting MAPKs-mediated inflammation in macrophages.International Immunopharmacology.2023, 119: 110066. 3. Du P, Hu T, An Z, et al. In vitro and in vivo synergistic efficacy of ceritinib combined with programmed cell death ligand‐1 inhibitor in anaplastic lymphoma kinase‐rearranged non‐small‐cell lung cancer. Cancer Science. 2020, 111(6): 1887. 4. Yang N, Zou C, Luo W, et al. Sclareol attenuates angiotensin II‐induced cardiac remodeling and inflammation via inhibiting MAPK signaling. Phytotherapy Research. 2022 5. Shi Y, Wang X, Meng Y, et al. A Novel Mechanism of Endoplasmic Reticulum Stress‐and c‐Myc‐Degradation‐Mediated Therapeutic Benefits of Antineurokinin‐1 Receptor Drugs in Colorectal Cancer. Advanced Science. 2021: 2101936. 6. Lu D, Zhang H, Zhang Y, et al. Secreted MbovP0145 Promotes IL-8 Expression through Its Interactive β-Actin and MAPK Activation and Contributes to Neutrophil Migration. Pathogens. 2021, 10(12): 1628. 7. Shen S, Wu G, Luo W, et al. Leonurine attenuates angiotensin II-induced cardiac injury and dysfunction via inhibiting MAPK and NF-κB pathway. Phytomedicine. 2022: 154519. 8. Sun B, Wu H, Lu J, et al. Irisin reduces bone fracture by facilitating osteogenesis and antagonizing TGF-β/Smad signaling in a growing mouse model of osteogenesis imperfecta. Journal of Orthopaedic Translation. 2023, 38: 175-189. 9. Wang D, Wang H, Yan Y, et al.Coating 3D-printed bioceramics with histatin promotes adhesion and osteogenesis of stem cells.Tissue Engineering.2023 (ja). 10. Lu D, Zhang H, Zhang Y, et al. Secreted MbovP0145 Promotes IL-8 Expression through Its Interactive β-Actin and MAPK Activation and Contributes to Neutrophil Migration. Pathogens 2021, 10, 1628. Pathogens. 2021

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Keywords

U0126 109511-58-2 Autophagy MAPK Mitophagy MEK MAP2K inhibit Inhibitor U 0126 Mitochondrial Autophagy U-0126 Influenza Virus MAPKK Mitogen-activated protein kinase kinase inhibitor

 

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