FX-11
Based on 33 publication(s) in Google Scholar
FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts.
For research use only. We do not sell to patients.
- Purity : 99.26%
- CAS No.: 213971-34-7
- Formula: C22H22O4
- Molecular Weight:350.41
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) FX-11
More- Cell Metab. 2021 Jan 5;33(1):51-64.e9. [Abstract]
- Cell Res. 2024 Jan;34(1):13-30. [Abstract]
- Immunity. 2024 Nov 12;57(11):2634-2650.e5. [Abstract]
- Gastroenterology. 2024 May;166(5):772-786.e14. [Abstract]
- Nat Metab. 2022 Dec;4(12):1830-1846. [Abstract]
- Autophagy. 2026 Jun 12:1-18. [Abstract]
- Nat Commun. 2025 Oct 10;16(1):9034. [Abstract]
- Adv Sci (Weinh). 2024 Oct;11(38):e2406333. [Abstract]
- J Transl Med. 2025 Oct 15;23(1):1105. [Abstract]
- Oncogene. 2026 May;45(17):1544-1556. [Abstract]
- Cell Chem Biol. 2026 Feb 19;33(2):213-226.e5. [Abstract]
- Free Radic Biol Med. 2025 Sep:237:503-514. [Abstract]
- J Anim Sci Biotechnol. 2024 May 10;15(1):68. [Abstract]
- Clin Transl Med. 2021 Jun;11(6):e467. [Abstract]
- Fundam Res. 2023 Mar 6;4(4):820-828. [Abstract]
- JCI Insight. 2026 Jun 8;11(11):e200928. [Abstract]
- Breast Cancer Res. 2024 Jun 7;26(1):96. [Abstract]
- Mol Cancer Res. 2025 Oct 17. [Abstract]
- Cell Oncol (Dordr). 2026 Jul 4.
- Int Immunopharmacol. 2026 Jul 13:186:117117.
- Int Immunopharmacol. 2025 Oct 10:163:115198. [Abstract]
- Int Immunopharmacol. 2024 Jan 5:126:111257. [Abstract]
- Biomolecules. 2022 Sep 4;12(9):1236. [Abstract]
- J Periodontal Res. 2025 Jan 29. [Abstract]
- Mol Med Rep. 2021 Feb;23(2):109. [Abstract]
- Sci Rep. 2023 Feb 24;13(1):3257. [Abstract]
- Exp Neurol. 2025 Sep:391:115318. [Abstract]
- J Cell Mol Med. 2025 Jul;29(13):e70692. [Abstract]
- FEBS J. 2025 Jun;292(12):3056-3071. [Abstract]
- bioRxiv. 2025 Sep 21.
- SSRN. 2023 Sep 7.
- bioRxiv. 2023 Jul 11.
- Universidad De Salamanca. 2023
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RT-PCR
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In Vivo Imaging
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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In Vivo Efficacy Study
Biological Activity
Description
IC50 & Target
IC50: 23.3 μM (LDHA in HeLa cell) [1].
In Vitro
FX-11 (9 μM, 24-48 h) shows activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase[2].
FX-11 (0-100 μM, 72 h) inhibits cell proliferation in BxPc-3 and MIA PaCa-2 cells[3].
FX-11 inhibits glycolysis and alters cellular energy metabolism in P493 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:P493 cells
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Concentration:9 μM
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Incubation Time:24 h, 48 h
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Result:Showed a decrease in ATP levels, accompanied by activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase.
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Cell Line:BxPc-3 and MIA PaCa-2 cells
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Concentration:0-100 µM
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Incubation Time:72 h
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Result:Reduced cell metabolic activity in a concentration-dependent manner, showed a significant reduction in cell proliferation, with IC50 values of 49.27 µM and 60.54 µM for BxPc-3 and MIA PaCa-2 cells, respectively.
In Vivo
FX-11 (0-2 mg/kg, IP, daily, for 3 weeks) significantly delays tumor growth[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SCID mice and RH-Foxn1nu mice (human P493 B-cell xenografts)[2]
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Dosage:42 µg/mouse (2.1 mg/kg)
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Administration:IP; daily for 10-14 days
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Result:Resulted in a remarkable inhibition of tumor growth, inhibited tumor xenograft progression.
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Animal Model:Immunocompromised CD-1 mice (6-8 weeks; 20-25 g, n=5 per group)[3]
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Dosage:2 mg/kg, 1 mg/kg+15 mg/kg TEPP-46, 2 mg/kg+30 mg/kg TEPP-46
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Administration:IP (100 µL), daily, for 3 weeks
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Result:Significantly lowered LDHA activity in plasma and tumor lysates; significantly lowered the expression of the proliferation marker Ki-67; significantly decreased proliferation indices were observed in tumor sections; significantly delayed tumor growth.
Chemical Information
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CAS No. 213971-34-7
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Appearance Solid
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Molecular Weight 350.41
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Formula C22H22O4
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Color White to off-white
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SMILES
O=C(C1=C2C=C(CC3=CC=CC=C3)C(C)=CC2=C(CCC)C(O)=C1O)O
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Synonyms
LDHA Inhibitor FX11
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Publications (33)
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Journal Impact Factor
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Most Recent
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Cell Metab
Metabolic-Pathway-Based Subtyping of Triple-Negative Breast Cancer Reveals Potential Therapeutic Targets. [Abstract]2021 Jan 5;33(1):51-64.e9. PMID: 33181091
FX-11 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 Jan 5;33(1):51-64.e9. [Abstract]
Dose-response curves for FX-11 (0-100 μM; 72 hours). Results of cell viability assays in five organoid models derived from TNBC patients.
FX-11 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 Jan 5;33(1):51-64.e9. [Abstract]
FX-11 (11.1 μM; 5–6 days). Representative bright-field images of organoids from three selected cases after drug treatment.
FX-11 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 Jan 5;33(1):51-64.e9. [Abstract]
The effect of anti-LDH antibody FX-11 (2 mg/kg; twice a week for 24 days) combined with immune checkpoint inhibitor therapy on TS/A tumor growth.
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Cell Res
2024 Jan;34(1):13-30. PMID: 38163844 -
Immunity
Inhibitory co-receptor Lag3 supports Foxp3+ regulatory T cell function by restraining Myc-dependent metabolic programming. [Abstract]2024 Nov 12;57(11):2634-2650.e5. PMID: 39236718 -
Gastroenterology
2024 May;166(5):772-786.e14. PMID: 38272100 -
Nat Metab
Metabolic enzyme LDHA activates Rac1 GTPase as a noncanonical mechanism to promote cancer. [Abstract]2022 Dec;4(12):1830-1846. PMID: 36536137
FX-11 purchased from MedChemExpress. Usage Cited in: Nat Metab. 2022 Dec;4(12):1830-1846. [Abstract]
FX11(1 mg/kg/day; i.p.) in combination with NSC23766 (NSC; 1.5 mg/kg/day; i.p.) for 2-3 weeks, displays a pronounced inhibitory effect on lung metastasis of Hs578T cells .
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Autophagy
H3K18la- driven neutrophil secretory autophagy promotes pulmonary endothelial dysfunction in sepsis-induced lung injury. [Abstract]2026 Jun 12:1-18. PMID: 42283498 -
Nat Commun
Histone lactylation promotes rheumatoid arthritis progression by increasing NFATc2 expression and the production of anti-lactylated histone autoantibodies. [Abstract]2025 Oct 10;16(1):9034. PMID: 41073397 -
Adv Sci (Weinh)
Lactylated Apolipoprotein C-II Induces Immunotherapy Resistance by Promoting Extracellular Lipolysis. [Abstract]2024 Oct;11(38):e2406333. PMID: 38981044 -
J Transl Med
Lactylation-induced ALKBH5 targets RNF123 to worsen retinal Müller cell activation through PKM2-regulated Glycolysis in diabetic retinopathy. [Abstract]2025 Oct 15;23(1):1105. PMID: 41094513 -
Oncogene
LDHA-driven lactate metabolism promotes MDSC activation and immunosuppressive microenvironment in prostate cancer. [Abstract]2026 May;45(17):1544-1556. PMID: 41922574 -
Cell Chem Biol
2026 Feb 19;33(2):213-226.e5. PMID: 41643668 -
Free Radic Biol Med
p67phox/NOX2 inhibits psoriasis by regulating the HIF-1α-glycolysis axis via p53-AMPK in keratinocytes. [Abstract]2025 Sep:237:503-514. PMID: 40516795 -
J Anim Sci Biotechnol
Proteo-transcriptomic profiles reveal key regulatory pathways and functions of LDHA in the ovulation of domestic chickens (Gallus gallus). [Abstract]2024 May 10;15(1):68. PMID: 38725063 -
Clin Transl Med
Functional inhibition of lactate dehydrogenase suppresses pancreatic adenocarcinoma progression. [Abstract]2021 Jun;11(6):e467. PMID: 34185423 -
Fundam Res
Astrocytic pyruvate dehydrogenase kinase-lactic acid axis involvement in glia-neuron crosstalk contributes to morphine-induced hyperalgesia in mice. [Abstract]2023 Mar 6;4(4):820-828. PMID: 39161415 -
JCI Insight
Lactate programs CRIP1 protein lactylation to drive synovial proliferation in rheumatoid arthritis. [Abstract]2026 Jun 8;11(11):e200928. PMID: 42258744 -
Breast Cancer Res
2024 Jun 7;26(1):96. PMID: 38849928 -
Mol Cancer Res
Bone Metastatic Progression of Prostate Cancer is Regulated by TRIM28-LDHA Mediated Metabolism. [Abstract]2025 Oct 17. PMID: 41105391 -
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Int Immunopharmacol
GDF15 attenuates sepsis-induced acute lung injury by suppressing the HIF-1α/LDHA pathway. [Abstract]2025 Oct 10:163:115198. PMID: 40669249 -
Int Immunopharmacol
NMAAP1 regulated macrophage polarizion into M1 type through glycolysis stimulated with BCG. [Abstract]2024 Jan 5:126:111257. PMID: 37988910 -
Biomolecules
4-OI Protects MIN6 Cells from Oxidative Stress Injury by Reducing LDHA-Mediated ROS Generation. [Abstract]2022 Sep 4;12(9):1236. PMID: 36139075 -
J Periodontal Res
A Novel Gene DUSP8 Missense Mutation Causes Nonsyndromic Hereditary Gingival Fibromatosis by Dysregulating Lysine Lactylation. [Abstract]2025 Jan 29. PMID: 39887402 -
Mol Med Rep
hCINAP serves a critical role in hypoxia‑induced cardiomyocyte apoptosis via modulating lactate production and mitochondrial‑mediated apoptosis signaling. [Abstract]2021 Feb;23(2):109. PMID: 33300073 -
Sci Rep
Bovine tumor necrosis factor-alpha Increases IL-6, IL-8, and PGE2 in bovine fibroblast-like synoviocytes by metabolic reprogramming. [Abstract]2023 Feb 24;13(1):3257. PMID: 36828912
FX-11 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2023 Feb 24;13(1):3257. [Abstract]
FX11 (20 μM; pretreat for 1 h) decreases bTNF-α-induced COX-2 mRNA expression and PGE2 synthesis in bovine fibroblast-like synoviocyte.
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Exp Neurol
Lactate exacerbates neuroinflammation in sepsis-associated encephalopathy via promoting neutrophil migration from skull bone marrow to the meninge. [Abstract]2025 Sep:391:115318. PMID: 40409661 -
J Cell Mol Med
Identification of LDHA as a Potential Therapeutic Target for Pulmonary Hypertension Through Modulation of Endothelial-To-Mesenchymal Transition. [Abstract]2025 Jul;29(13):e70692. PMID: 40629253 -
FEBS J
Sex-related changes in lactate dehydrogenase A expression differently impact the immune response in melanoma. [Abstract]2025 Jun;292(12):3056-3071. PMID: 39888245 -
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Solvent & Solubility
In Vitro:
DMSO : 250 mg/mL (713.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
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 U S A. 2010 Feb 2;107(5):2037-42. [Content Brief]
[3]. 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 Sep 16;11(9):1372. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8538 mL | 14.2690 mL | 28.5380 mL | 71.3450 mL |
| 5 mM | 0.5708 mL | 2.8538 mL | 5.7076 mL | 14.2690 mL | |
| 10 mM | 0.2854 mL | 1.4269 mL | 2.8538 mL | 7.1345 mL | |
| 15 mM | 0.1903 mL | 0.9513 mL | 1.9025 mL | 4.7563 mL | |
| 20 mM | 0.1427 mL | 0.7134 mL | 1.4269 mL | 3.5672 mL | |
| 25 mM | 0.1142 mL | 0.5708 mL | 1.1415 mL | 2.8538 mL | |
| 30 mM | 0.0951 mL | 0.4756 mL | 0.9513 mL | 2.3782 mL | |
| 40 mM | 0.0713 mL | 0.3567 mL | 0.7134 mL | 1.7836 mL | |
| 50 mM | 0.0571 mL | 0.2854 mL | 0.5708 mL | 1.4269 mL | |
| 60 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 1.1891 mL | |
| 80 mM | 0.0357 mL | 0.1784 mL | 0.3567 mL | 0.8918 mL | |
| 100 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.7134 mL |