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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
规格:98%
分子量:350.41
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
FX-11 (LDHA Inhibitor FX11) was found to be a potent, competitive inhibitor of the human LDH-A's NADH binding pocket.
货号:ajcx13116
CAS:213971-34-7
分子式:C22H22O4
分子量:350.41
溶解度:DMSO: 250 mg/mL (713.45 mM)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

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].

参考文献:
[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

Protocol:

Cell experiment [1]:

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 experiment [2]:

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.

参考文献:

[1]: 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.
[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).