產(chǎn)品說明
STAT3抑制劑
該產(chǎn)品包含在以下化合物庫中:
質(zhì)量控制
化學(xué)性質(zhì)
| CAS號(hào) | 22112-89-6 | ? | ? |
| 別名 | 5,15-Diphenylporphyrin,STAT3 Inhibitor VIII |
| 分子式 | C32H22N4 | 分子量 | 462.6 |
| 溶解性 | Soluble in DMSO | 儲(chǔ)存條件 | Store at -20° |
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實(shí)驗(yàn)操作
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產(chǎn)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.
溫馨提示：不可用于臨床治療。