KC7F2

KC7F2

Catalog Number:
L002369263APE
Mfr. No.:
APE-A4507
Price:
$201
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      • Overview
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          Background

          KC7F2 is a novel inhibitor of HIF-1αwith IC50 value of 20 μM [1].
          Hypoxia inducible factor-1 (HIF-1) is a heterodimeric transcription factor consisting of α and β subunits. In normal situation, the HIF-1α subunit is constitutively translated, but rapidly degraded. While, under hypoxia it is stabilized. HIF target genes encode a series of critical factors to adapt the low oxygen [1].
          In a HIF-reporter cell line LN229-HRE-AP, KC7F2 (>25 μM) reduced AP activity by 90% in LN229 cells, which indicated that KC7F2 inhibited AP enzyme activity. In LNZ308 human glioma cells, KC7F2 inhibited the expression of a panel of HIF target genes, such as matrix metalloproteinase 2 (MMP2), enolase 1, carbonic anhydrase IX (CA IX) and endothelin 1. Also, KC7F2 reduced expression of HIF-1α in a dose-dependent way [1].
          In a rat epilepsy model, KC7F2 significantly shortened the latent period in the PTZ kindling model and increased the rate of spontaneous recurrent seizures during the chronic stage in the lithium-pilocarpine model [3].

          [1]. Narita T, Yin S, Gelin CF, et al. Identification of a novel small molecule HIF-1alpha translation inhibitor. Clin Cancer Res, 2009, 15(19): 6128-6136.
          [2]. Li J, Jiang G, Chen Y, et al. Altered expression of hypoxia-Inducible factor-1α participates in the epileptogenesis in animal models. Synapse, 2014, 68(9): 402-409.

      • Properties
        • Alternative Name
          2,5-dichloro-N-[2-[2-[(2,5-dichlorophenyl)sulfonylamino]ethyldisulfanyl]ethyl]benzenesulfonamide
          CAS Number
          927822-86-4
          Molecular Formula
          C16H16Cl4N2O4S4
          Molecular Weight
          570.38
          Appearance
          A solid
          Purity
          99.56%
          Solubility
          ≥24.95 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Na Jiang, Hao Zhao, et al. "HIF‐1α ameliorates tubular injury in diabetic nephropathy via HO‐1–mediated control of mitochondrial dynamics." Cell Prolif. 2020 Nov;53(11):e12909. PMID:32975326
          2. Chen Z, Tian D, et al. "Apigenin Combined With Gefitinib Blocks Autophagy Flux and Induces Apoptotic Cell Death Through Inhibition of HIF-1α, c-Myc, p-EGFR, and Glucose Metabolism in EGFR L858R+T790M-Mutated H1975 Cells." Front Pharmacol. 2019 Mar 22;10:260. PMID:30967777

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