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FX-11(LDHA Inhibitor FX11)
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。
FX-11(LDHA Inhibitor FX11)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
FX-11 (LDHA Inhibitor FX11) 是一种有效的、选择性的、可逆的和竞争性的乳酸脱氢酶 A (LDHA) 特异性抑制剂,Ki 为 8 μM. FX-11(LDHA Inhibitor FX11)能有效激活PKM2(丙酮酸激酶M2)。 FX-11 (LDHA Inhibitor FX11) 降低 ATP 水平并诱导氧化应激、ROS 产生和细胞死亡。 FX-11 (LDHA Inhibitor FX11) 在淋巴瘤和胰腺癌异种移植物中显示出抗肿瘤活性。

Cell lines

PC3 and DU145 (prostate carcinoma) cell lines

Preparation Method

PC3 and DU145 cells maintained in log phase growth were plated in 96-well plates and treated with 0.25, 0.5, 1.5, 5, 15, 30, 60, 120, and 240 μmol/L FX-11 for 24 hours.

Reaction Conditions

0.25, 0.5, 1.5, 5, 15, 30, 60, 120, and 240 μmol/L for 24 hours

Applications

After treated with FX-11, the metabolic phenotype of the two cell lines in vitro demonstrated no significant difference in extracellular acidification rate (ECAR), oxygen consumption rate (OCR), pyruvate uptake, and lactate production.

Animal models

male SCID mice

Preparation Method

groups of five mice were injected with control 2% (vol/vol) DMSO or 42 μg of FX11

Dosage form

Intraperitoneal injection, 42μg daily, for 10 days

Applications

Daily i.p. injection of 42 μg of FX11 also resulted in a remarkable inhibition of tumor growth.

产品描述

FX-11 (LDHA Inhibitor FX11) was found to be a potent, competitive inhibitor of the human LDH-A's NADH binding pocket[1]. FX-11 was recharacterized using purified human liver LDHA with Ki of 8μM[2]FX11 inhibition of LDHA increased nonproductive mitochondrial respiration, leading to decreased ATP levels and cell proliferation, and increased oxygen consumption, ROS production and cell death[5].

FX-11 (IC50) for proliferation of DU145 and PC3 (prostate carcinoma) cell lines in vitro was strikingly similar (32 ± 1.1 μmol/L vs. 27 ± 1.1 μmol/L, respectively)[3]. Low concentrations of FX-11 could markedly decrease cell viability in the MPS2(the glycolytic subtype with upregulated carbohydrate and nucleotide metabolism) PDO (Patient-derived organoid) models[4].

FX-11, effectively inhibited tumor growth in human B-lymphoma and pancreatic cancer xenograft models. FX-11 could inhibit tumor growth in P493 lymphomas and human P198 pancreatic tumors ≥200 mm3[5].

References:
[1]. EC Calvaresi. Small molecule inhibitors of lactate dehydrogenase a as an anticancer strategy. 2014.
[2]: Le, A. et al. Inhibition of lactate dehydrogenase A induces oxidative stress and inhibits tumor progression. Proc. Natl Acad. Sci. USA 107, 2037-2042 (2010).
[3]. Scroggins BT, Matsuo M, White AO, et al. Hyperpolarized [1-13C]-pyruvate magnetic resonance spectroscopic imaging of prostate cancer In Vivo predicts efficacy of targeting the Warburg effect. Clin Cancer Res 2018;24(13):3137-3148.
[4]. Gong Y, Ji P, Yang Y-S, Xie S, Yu T-J, Xiao Y, et al. Metabolic-Pathway-Based Subtyping of Triple-Negative Breast Cancer Reveals Potential Therapeutic Targets. Cell Metab (2021) 33:51-64.e9. doi: 10.1016/j.cmet.2020.10.012
[5]. P. Miao, S. Sheng, X. Sun, J. Liu, G. Huang.Lactate dehydrogenase A in cancer: a promising target for diagnosis and therapy. IUBMB Life, 65 (11) (2013), pp. 904-910