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PRL-3 Inhibitor I

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Chemical Structure| 893449-38-2 同义名 : BR-1;Compound 5e;PTP4A3 Inhibitor;Phosphatase of Regenerating Liver 3 Inhibitor;P0108;PRL-3 Inhibitor
CAS号 : 893449-38-2
货号 : A1166385
分子式 : C17H11Br2NO2S2
纯度 : 98%
分子量 : 485.213
MDL号 : MFCD11045303
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(82.44 mM)，配合低频超声，并水浴加热至45℃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
动物实验配方：
生物活性
描述 PRL-3 is a member of phosphatases of regenerating liver family, characterized by phosphatase active domain and C-terminal prenylation motif. Overexpression of PRL-3 has been implicated in multiple cancers[3]. In gastric cancer cells, PRL-3 upregulated miR-210 expression in a HIF-1α-dependent fashion under normoxia and hypoxia. In addition, PRL-3 activated NF-κB signaling and promoted HIF-1α expression through modulating phosphorylation of p65. NF-κB signaling, HIF-1α, and miR-210 partially contributed to PRL-3-induced migration and invasion[4]. Knockdown of PRL-3 in MCF-7 cells resulted in decreased proliferation, wound healing and invasion. PRL-3 knockdown in MCF-7 cells resulted in a significant reduction of heparanase, MMP-9, actin gamma-2 and Myosin 9 expression, and significant elevation of E-cadherin[5]. BR-1 is a phosphatase of regenerating liver 3 (PRL-3) inhibitor which blocks the migration and invasion of metastatic cancer cells. PRL-3 inhibitor, in a dose-dependent fashion, blocked the dephosphorylation of DiFMUP by PRL-3 and strongly suppressed the activity of PRL-3 phosphatase in PRL-3 overexpressing DLD-1 colon tumor cells [DLD-1 (PRL-3)]. Also, PRL-3 inhibitor dose-dependently blocked the migration of DLD-1 (PRL-3) cells, however, it did not inhibit the proliferation of DLD-1(PRL-3) cells, suggesting that PRL-3 inhibitor significantly blocked cell immigration and invasion without cytotoxicity[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.30mL

2.06mL

1.03mL

20.61mL

4.12mL

2.06mL
参考文献

[1]Ahn JH, Kim SJ, Park WS, Cho SY, Ha JD, Kim SS, Kang SK, Jeong DG, Jung SK, Lee SH, Kim HM, Park SK, Lee KH, Lee CW, Ryu SE, Choi JK. Synthesis and biological evaluation of rhodanine derivatives as PRL-3 inhibitors. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2996-9. doi: 10.1016/j.bmcl.2006.02.060. Epub 2006 Mar 10. PMID: 16530413.

[2]Tian W, Qu L, Meng L, Liu C, Wu J, Shou C. Phosphatase of regenerating liver-3 directly interacts with integrin β1 and regulates its phosphorylation at tyrosine 783. BMC Biochem. 2012 Oct 23;13:22. doi: 10.1186/1471-2091-13-22. PMID: 23092334; PMCID: PMC3558359.

[3] Xiaofang Xing,et al. Phosphatase of regenerating liver-3 (PRL-3) is associated with metastasis and poor prognosis in gastric carcinoma. J Transl Med. 2013 Dec 13;11:309.

[4]Cheng Zhang,et al. PRL-3 promotes gastric cancer migration and invasion through a NF-κB-HIF-1α-miR-210 axis. J Mol Med (Berl). 2016 Apr;94(4):401-15.

[5]Isabel Radke,et al. Expression of PRL-3 regulates proliferation and invasion of breast cancer cells in vitro. Arch Gynecol Obstet. 2017 Dec;296(6):1153-1160.

[6]Min G , Lee S K , Kim H N , et al. Rhodanine-based PRL-3 inhibitors blocked the migration and invasion of metastatic cancer cells[J]. Bioorganic & Medicinal Chemistry Letters, 2013, 23(13):3769-3774.