BAY 87-2243

BAY 87-2243

Catalog Number:
L002369822APE
Mfr. No.:
APE-B1115
Price:
$378
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      • Overview
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          Background

          BAY 87-2243 is a selective inhibitor of HIF-1 induced gene activation [1].In HCT-116 cells, BAY 87-2243 inhibits the hypoxia increased HRE-dependent luciferase expression with IC50 value of 0.7nM and inhibits the expression of HIF target gene CA9 with IC50 value of 2nM. In H460 cells cultured under hypoxia, BAY 87-2243 suppresses the expression of HIF-1 target genes including CA9, adrenomedullin and angiopoietin-like protein-4. BAY 87-2243 also inhibits both HIF-1α and HIF-2α protein accumulation in this cell line. Moreover, in mice model bearing H460 xenograft, treatment of BAY 87-2243 reduces the expression levels of HIF-1 target genes CA9, ANGPTL4 and EGLN3 and meanwhile reduces the tumor weight. In addition, BAY 87-2243 is also found to act as an inhibitor of mitochondrial function. It can inhibit the oxygen consumption with IC50 value of 10nM [1].

          [1] Ellinghaus P, Heisler I, Unterschemmann K, et al. BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. Cancer medicine, 2013, 2(5): 611-624.

      • Properties
        • Alternative Name
          5-(1-((2-(4-cyclopropylpiperazin-1-yl)pyridin-4-yl)methyl)-5-methyl-1H-pyrazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole
          CAS Number
          1227158-85-1
          Molecular Formula
          C26H26F3N7O2
          Molecular Weight
          525.53
          Appearance
          A solid
          Purity
          99.85%
          Solubility
          insoluble in H2O; ≥8.24 mg/mL in EtOH with ultrasonic; ≥8.76 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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