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FX-11

FX-11 (LDHA Inhibitor FX11) 是一种有效的、选择性的和竞争性的乳酸脱氢酶 A (LDHA) 的特异性抑制剂，对LDHA 的Ki 为 8 μM。FX-11 对PKM2 (丙酮酸激酶 M2)具有激活作用。FX-11 可降低 ATP 水平，诱导氧化应激和ROS 生成，可引起细胞死亡。FX-11 在淋巴瘤和胰腺癌异种移植过程中表现出抗肿瘤 活性。

CAS号

213971-34-7

分子式

C22H22O4

主要靶点

Dehydrogenase

仅限科研使用

Cat No : CM11586

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Synonyms

LDHA Inhibitor FX11

验证数据展示

  • CAS No.: 213971-34-7

    FX-11
    CAS#: 213971-34-7

产品信息

FX-11 is A potent, selective and competitive specific inhibitor of lactate dehydrogenase A (LDHA) with a Ki of 8 μM. FX-11 can activate PKM2 (pyruvate kinase M2). FX-11 can reduce ATP levels, induce oxidative stress and ROS production, and cause cell death. FX-11 appeared antitumor activity during xenotransplantation of lymphoma and pancreatic cancer.

CAS号 213971-34-7
分子式 C22H22O4
主要靶点 Dehydrogenase
主要通路 代谢
分子量 350.41
纯度 98.95%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 LDHA Inhibitor FX11

靶点活性

LDHA:8 μM(Ki)|LDHA, HeLa cell:23.3 μM|LDHA(HeLa cell):23.3 μM|DU145(cell):32 ± 1.1 μM|PC3(cell):27 ± 1.1 μM

体内活性

FX-11 (42 µg/mouse; IP, administered daily for 10-14 days) suppresses P493 tumor growth.[1] FX-11 (0-2 mg/kg, IP, daily, for 3 weeks) notably retards tumor growth.[2]

体外活性

FX-11 (9 μM, 24-48 h) induces activation of AMP kinase and phosphorylation of acetyl-CoA carboxylase, its substrate. FX-11 disrupts glycolysis and modifies cellular energy metabolism in P493 cells. [1] FX-11 (0-100 µM, 72 h) impedes cell proliferation in BxPc-3 and MIA PaCa-2 cells. [2]

溶解度

DMSO:225.0 mg/mL (642.1 mM),Sonification is recommended.

参考文献

1.Le A, et al. Inhibition of lactate dehydrogenase A induces oxidative stress and inhibits tumor progression. Proc Natl Acad Sci U S A. 2010;107(5):2037-204
2.Mohammad GH, et al. Targeting Pyruvate Kinase M2 and Lactate Dehydrogenase A Is an Effective Combination Strategy for the Treatment of Pancreatic Cancer. Cancers (Basel). 2019;11(9):137
3.Scroggins BT, 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, et al. Metabolic-Pathway-Based Subtyping of Triple-Negative Breast Cancer Reveals Potential Therapeutic Targets. Cell Metab. 2021;33(1):51-64.

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