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5,15-DPP
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
5,15-DPP图片
CAS NO:22112-89-6
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议

产品介绍
5,15-DPP (5,15-DPP) 是一种选择性 STAT3-SH2 拮抗剂(对于 STAT3 和 STAT1,IC50 分别为 0.28 ⋼;M 和 10 μ;M)。
Cas No.22112-89-6
别名5,15-二苯基-21H,23H-卟吩,5,15-Diphenylporphyrin,STAT3 Inhibitor VIII
化学名5,15-diphenyl-21H,23H-porphine
Canonical SMILESC1(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
分子式C32H22N4
分子量462.6
溶解度≤2mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.