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Synonyms: LDHA Inhibitor FX11


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $41 | In Stock | In Stock | |
| 5 mg | $98 | In Stock | In Stock | |
| 10 mg | $142 | In Stock | In Stock | |
| 25 mg | $236 | In Stock | In Stock | |
| 50 mg | $348 | In Stock | In Stock | |
| 100 mg | $520 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $107 | In Stock | In Stock |
| Description | FX-11 (LDHA Inhibitor FX11) is a highly potent, selective, and competitive inhibitor of lactate dehydrogenase A (LDHA), with a Ki value of 8 μM for LDHA. FX-11 acts as an activator of PKM2 (pyruvate kinase M2). FX-11 exerts its antitumor effects by inhibiting glycolysis, depleting ATP, and inducing oxidative stress and apoptosis. FX-11 can be used in tumor metabolism research. |
| Targets & IC50 | LDHA:8 μM (Ki), LDHA (HeLa cells):23.3 μM, PC3 cells:27 ± 1.1 μM, DU-145 cells:32 ± 1.1 μM |
| In vitro | Methods: Human breast cancer cells (MCF-7) were cultured under normoxic and hypoxic conditions. Cells were treated with the inhibitor FX-11 at half-logarithmic dilution concentrations (200, 100, 50, 25, 12.5, 0 μM) for 24 hours. Cell viability was assessed using the AlamarBlue assay. Results: FX-11 monotherapy: Inhibited cancer cell proliferation under both normoxic and hypoxic conditions. [1] Methods: Human umbilical vein endothelial cells (HUVEC) were treated with FX-11 (20 μM). After 2 hours, cells were stimulated with LPS (200 ng/mL) for 24 hours to induce inflammation. Immunoblotting was used to detect HIF-1α and LDHA expression levels. Results: FX-11 treatment significantly suppressed LPS-induced upregulation of HIF-1α and LDHA protein expression. [2] |
| In vivo | Methods: C57BL/6J mice were administered FX-11 (10 mg/kg) via intraperitoneal injection. Two hours later, LPS (20 mg/kg) was administered intraperitoneally to induce an acute lung injury model of sepsis. Tissue samples were collected and analyzed after 24 hours. Results: FX-11 pretreatment significantly attenuated LPS-induced pathological damage in lung tissue and markedly reduced HIF-1α and LDHA protein levels in lung tissue. [2] |
| Synonyms | LDHA Inhibitor FX11 |
| Molecular Weight | 350.41 |
| Formula | C22H22O4 |
| Cas No. | 213971-34-7 |
| Smiles | CCCc1c(O)c(O)c(C(O)=O)c2cc(Cc3ccccc3)c(C)cc12 |
| Relative Density. | 1.260 g/cm3 (Predicted) |
| Storage | Store at low temperature,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 260 mg/mL (741.99 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (14.27 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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