5,15-DPP
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].
References:
[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.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 462.6 |
| Cas No. | 22112-89-6 |
| Formula | C32H22N4 |
| Synonyms | 5,15-Diphenylporphyrin,STAT3 Inhibitor VIII |
| Solubility | ≤2mg/ml in dimethyl formamide |
| Chemical Name | 5,15-diphenyl-21H,23H-porphine |
| SDF | Download SDF |
| Canonical SMILES | C1(C=C/2)=NC2=C/C3=CC=C(/C(C4=CC=CC=C4)=C5N=C(/C=C6N/C(C=C\6)=C1/C7=CC=CC=C7)C=C\5)N3 |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Quality Control & MSDS
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Chemical structure
