Galloflavin

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Chemical Structure| 568-80-9 同义名 : NSC 107022
CAS号 : 568-80-9
货号 : A477947
分子式 : C12H6O8
纯度 : 99%+
分子量 : 278.17
MDL号 : MFCD26941292
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Lactate dehydrogenase (LDH) is an essential metabolic enzyme that catalyzes the interconversion of pyruvate and lactate using NADH/NAD(+) as a co-substrate. Many cancer cells exhibit a glycolytic phenotype known as the Warburg effect, in which elevated LDH levels enhance the conversion of glucose to lactate, making LDH an attractive therapeutic target for oncology[1]. Galloflavin inhibits both the A and B isoforms of lactate dehydrogenase with Ki of 5.46 µM and 15.06 µM, respectively. Galloflavin is also a potential anticancer agent[2]. Galloflavin and Ellagic acid showed anti-proliferative effects on Caco2. The compounds also upregulated SIRT6 expression whereas key proteins in glycolysis were downregulated. Galloflavin decreased glucose transporter 1 (GLUT1) expression, and Ellagic acid affected the expression of protein dehydrogenase kinase 1 (PDK1)[3]. Galloflavin reduced PDAC proliferation in monoculture (P < 0.01); however, in co-culture with PSCs, an antiproliferative effect was only evident in PANC-1 (P = 0.001). An apoptotic effect was observed in MIA PaCa-2 and BxPC-3 in coculture (P < 0.05). A reduction in media lactate was observed in coculture (P < 0.01) with PSCs. Immunohistochemistry revealed stromal and tumoral LDHB expression had no impact on survival[4].Galloflavin effectively inhibited cell growth in endometrial cancer cell lines and primary cultures of human endometrial cancer through its involvement in multiple signaling pathways that regulate metabolism, cell cycle, apoptosis, cell stress and metastasis[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.59mL

0.72mL

0.36mL

17.97mL

3.59mL

1.80mL

35.95mL

7.19mL

3.59mL
参考文献

[1]Subramaniapillai Kolappan,et al. Structures of lactate dehydrogenase A (LDHA) in apo, ternary and inhibitor-bound forms. Acta Crystallogr D Biol Crystallogr. 2015 Feb;71(Pt 2):185-95.

[2] 1. Manerba M, Vettraino M, Fiume L, Di Stefano G, Sartini A, Giacomini E, Buonfiglio R, Roberti M, Recanatini M. Galloflavin (CAS 568-80-9): a novel inhibitor of lactate dehydrogenase. ChemMedChem. 2012 Feb 6;7(2):311-7.

[3] Minna Rahnasto-Rilla,et al. Effects of galloflavin and ellagic acid on sirtuin 6 and its anti-tumorigenic activities. Biomed Pharmacother. 2020 Nov;131:110701.

[4]John A G Moir,et al. Therapeutic Strategies Toward Lactate Dehydrogenase Within the Tumor Microenvironment of Pancreatic Cancer. Pancreas.Nov/Dec 2020;49(10):1364-1371.

[5]Xiaoyun Han,et al. Evaluation of the anti-tumor effects of lactate dehydrogenase inhibitor galloflavin in endometrial cancer cells. J Hematol Oncol. 2015 Jan 29;8:2.