U0126-EtOH

U0126-EtOH

Catalog Number:
L002368298APE
Mfr. No.:
APE-A1337
Price:
$188
  • Size:
    Quantity:
    Add to Cart:
      • Overview
        • Please contact us at for specific academic pricing.

          Background

          U0126-EtOH is a selective inhibitor of MEK1 and MEK2 with IC50 values of 70 nM and 60 nM, resepctively [1].
          U0126 was screened out as an anti-inflammatory agent that inhibited AP-1 transcription with IC50 value of 1μM and had no interactions with GREs. U0126 binds MEK1/2 in a unique site. This inhibition of MEK1/2 is noncompetitive with ERK and ATP. U0126 showed no effects on other MAPKKs. In HT22 cells, U0126 treatment significantly inhibited the cell injury caused by oxidative glutamate toxicity and remarkably blocked the phosphorylation of ERK1/2. Besides that, U0126 exerted no neuroprotection against other stimuli such as TNFα and actinomycin D. U0126 treatment also protected the primary cultured cortical neurons from oxidative glutamate toxicity and hypoxia/reoxygenation [1, 2].

          [1] Duncia J V, Santella III J B, Higley C A, et al. MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorganic & Medicinal Chemistry Letters, 1998, 8(20): 2839-2844.
          [2] Satoh T, Nakatsuka D, Watanabe Y, et al. Neuroprotection by MAPK/ERK kinase inhibition with U0126 against oxidative stress in a mouse neuronal cell line and rat primary cultured cortical neurons. Neuroscience letters, 2000, 288(2): 163-166.

      • Properties
        • Alternative Name
          (2Z,3Z)-2,3-bis[amino-(2-aminophenyl)sulfanylmethylidene]butanedinitrile;ethanol
          CAS Number
          1173097-76-1
          Molecular Formula
          C18H16N6S2·C2H6O
          Molecular Weight
          426.56
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥21.33 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Danhui Liu, Yuzhen Liu, et al. "Trichostatin A promotes esophageal squamous cell carcinoma cell migration and EMT through BRD4/ERK1/2-dependent pathway." Cancer Med. 2021 Aug;10(15):5235-5245. PMID:34160902
          2. Xiaoli Liu, Yan Gu, et al. "Honokiol induces paraptosis-like cell death of acute promyelocytic leukemia via mTOR & MAPK signaling pathways activation." Apoptosis. 2021 Apr;26(3-4):195-208. PMID:33550458
          3. Ha SD, Cho W, et al. "The transcription factor PU.1 mediates enhancer-promoter looping that is required for IL-1β eRNA and mRNA transcription in mouse melanoma and macrophage cell lines." J Biol Chem. 2019 Nov 15;294(46):17487-17500. PMID:31586032
          4. Liu W, Zhan C, et al. "Microcystin-LR influences the in vitro oocyte maturation of zebrafish by activating the MAPK pathway." Aquat Toxicol. 2019 Oct;215:105261. PMID:31419757
          5. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May
          6;49(3):425-443.e9. PMID:31063758
          6. Huang SZ, Wei MN, et al. "Targeting TF-AKT/ERK-EGFR Pathway Suppresses the Growth of Hepatocellular Carcinoma." Front Oncol. 2019 Mar 15;9:150. PMID:30931258
          7. Wang Q, Zhou C, et al. "The involvement of the ERK-MAPK pathway in TGF-β1-mediated connexin43-gap junction formation in chondrocytes. Connect Tissue Res." 2019 Mar 22:1-10. PMID:30897973
          8. Vincent Picher-Martel. "L’implication de l’ubiquiline-2 dans l’agrégation de TDP-43 et la pathogénèse de la sclérose latérale amyotrophique." University Laval. 2019.
          9. Chen M, Ye K, et al. "Paris Saponin II inhibits colorectal carcinogenesis by regulating mitochondrial fission and NF-κB pathway." Pharmacol Res. 2018 Nov 22;139:273-285. PMID:30471409
          10. Zhu Y, Li Q, et al. "TLR activation inhibits the osteogenic potential of human periodontal ligament stem cells through Akt signaling in a Myd88- or TRIF-dependent manner." J Periodontol. 2018 Oct 26. PMID:30362568
          11. MXinwei Feng1, Junfeng Lu2, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.
          12. Lu YT, Li LZ, et al."Succinate induces aberrant mitochondrial fission in cardiomyocytes through GPR91 signaling." Cell Death Dis. 2018 Jun 4;9(6):672. PMID:29867110
          13. Ma L, Jiang Y, et al. "Anti-TNF-alpha antibody attenuates subarachnoid hemorrhage-induced apoptosis in the hypothalamus by inhibiting the activation of Erk." Neuropsychiatr Dis Treat. 2018 Feb 15;14:525-536. PMID:29497296
          14. Sieber J, Wieder N, et al. "GDC-0879, a BRAF(V600E) Inhibitor, Protects Kidney Podocytes from Death." Cell Chem Biol. 2017 Dec 6. PMID:29249695
          15. Wang HY, Wang W, et al. "Role of KCNB1 in the prognosis of gliomas and autophagy modulation." Sci Rep. 2017 Feb 8;7(1):14. PMID:28144039

    Note: If you don't receive our verification email, do the following:

    Copyright © Amerigo Scientific. All rights reserved.