产品说明书

TMPyP4 tosylate

Print
Chemical Structure| 36951-72-1 同义名 : TMP 1363;TMPyP4 (tosylate);TMP-1363 tetratosylate;TMPyP4 4-methylbenzenesulfonate
CAS号 : 36951-72-1
货号 : A246194
分子式 : C72H66N8O12S4
纯度 : 98%+
分子量 : 1363.6
MDL号 : MFCD00013468
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 9 mg/mL(6.56 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(3.65 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 The biological functions of G-quadruplexes are closely related to the binding of some proteins. Insulin-like growth factor type I (IGF-1), as a significant modulator of cell growth and development, may serve as a quadruplex-binding protein.TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1. IGF-1 shows a binding specificity for G-quadruplex structures, especially the G-quadruplex structure with a parallel topology. The quadruplex-specific ligands TMPyP4 and PDS (Pyridostatin) can inhibit the interaction between G-quadruplexes and proteins[1]. TMPyP4 is a cationic porphyrin that intercalates into and stabilizes G-quadruplexes, which are formed by DNA and RNA sequences composed of blocks of guanine residues[2]. TMPyP4 induces telomere shortening, and inhibition of the cell growth in HOS and Saos-2 with over 17% apoptosis rates.[3]. TMPyP4 inhibits telomerase activity (IC50 ≤ 50 µM), blocking the clonogenic growth and migration of cancer cells in culture and in vivo[4]. TMPyP4 potently suppressed cell viability and induced the apoptosis of SW480 cells in a dose-dependent manner. In addition, the downregulation of Wnt, β-catenin and cyclinD1 expression levels was detected in TMPyP4-treated SW480 cells.[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.73mL

0.15mL

0.07mL

3.67mL

0.73mL

0.37mL

7.33mL

1.47mL

0.73mL
参考文献

[1] Nithya Krishnamurthy,et al. Targeting the Wnt/beta-catenin pathway in cancer: Update on effectors and inhibitors. Cancer Treat Rev. 2018 Jan;62:50-60.

[2]Fiel, R.J., Howard, J.C., Mark, E.H., et al. Interaction of DNA with a porphyrin ligand: Evidence for intercalation. Nucleic Acids Res. 1979. 6(9), 3093-3118.

[3]Jun Fujimori,et al. Antitumor effects of telomerase inhibitor TMPyP4 in osteosarcoma cell lines. J Orthop Res. 2011. 29(11):1707-11.

[4]Rapozzi, V., Zorzet, S., Zacchigna, M., et al. Anticancer activity of cationic porphyrins in melanoma tumour-bearing mice and mechanistic in vitro studies. Mol. Cancer. 2014. 13, 75.

[5]Yi-Qiang Zhang,et al. TMPyP4-regulated cell proliferation and apoptosis through the Wnt/β-catenin signaling pathway in SW480 cells. J Recept Signal Transduct Res. 2016. 36(2), 167-72.