5,15-DPP

5,15-DPP

Catalog Number:
L002372914APE
Mfr. No.:
APE-C3975
Price:
$297
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      • Overview
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          Background

          5,15-diphenylporphyrin (5,15-DPP) is a selective STAT3-SH2 antagonist [1].
          Stat3 is constitutively activated in many human cancers. Stat3 functions as a critical mediator of oncogenic signaling through transcriptional activation of genes encoding apoptosis inhibitors, cell-cycle regulators and inducers of angiogenesis [2]. Aberrant STAT3 activity has been associated with transforming mechanisms induced by oncogenic tyrosine kinases [1].
          In vitro: 5,15-DPP directly bound to STAT3 and antagonized the function of STAT3-SH2. 5,15-DPP selectively antagonized STAT3-SH2 with an IC50 of 0.28 μM over the other SH2-containing proteins STAT1 and Grb2[1]. The estimated KD values for the 5,15-DPP binding to STAT3 was 880 nM. Treatment with 5,15-DPP suppressed the DNA binding activity of STAT3 in a concentration-dependent manner. 5,15-DPP poorly inhibited STAT1 with an IC50 of 10 μM and showed no effect Grb2 [1].

          [1] Uehara Y, Mochizuki M, Matsuno K, et al. Novel high-throughput screening system for identifying STAT3–SH2 antagonists[J]. Biochemical and biophysical research communications, 2009, 380(3): 627-631.
          [2] Jing N, Tweardy D J. Targeting Stat3 in cancer therapy[J]. Anti-cancer drugs, 2005, 16(6): 601-607.

      • Properties
        • Alternative Name
          5,15-Diphenylporphyrin,STAT3 Inhibitor VIII; 5,15-diphenyl-21H,23H-porphine
          CAS Number
          22112-89-6
          Molecular Formula
          C32H22N4
          Molecular Weight
          462.6
          Appearance
          A crystalline solid
          Purity
          Purity ≥95.00%
          Solubility
          ≤2mg/ml in dimethyl formamide
          Storage
          Store at -20°C

          * For Research Use Only

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