GSK2837808A
Based on 47 publication(s) in Google Scholar
GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 2.6 and 43 nM for hLDHA and hLDHB, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.24%
- CAS. Nr.: 1445879-21-9
- Formel: C31H25F2N5O7S
- Molecular Weight:649.62
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) GSK2837808A
More- Mol Cancer. 2026 Apr 2;25(1):130. [Abstract]
- Cell Metab. 2025 Apr 1;37(4):903-919.e10. [Abstract]
- Gastroenterology. 2024 Jan 24:S0016-5085(24)00064-7. [Abstract]
- Nat Commun. 2020 Jul 9;11(1):3427. [Abstract]
- Nat Commun. 2020 Jun 22;11(1):3162. [Abstract]
- Nat Commun. 2019 Jun 20;10(1):2701. [Abstract]
- Adv Sci (Weinh). 2024 Jul 15:e2404119. [Abstract]
- J Adv Res. 2025 Sep 26:S2090-1232(25)00756-8. [Abstract]
- J Exp Clin Cancer Res. 2021 Dec 10;40(1):390. [Abstract]
- Cell Death Dis. 2026 Jun 3. [Abstract]
- Cell Death Dis. 2025 Aug 25;16(1):642. [Abstract]
- Int J Biol Macromol. 2024 Oct 30:137070. [Abstract]
- Int J Biol Macromol. 2024 Jan;254(Pt 1):127629. [Abstract]
- Acta Pharmacol Sin. 2025 Jun 11. [Abstract]
- Int J Hydrogen Energy. 6 December 2021.
- J Transl Med. 2025 Aug 18;23(1):923. [Abstract]
- Stem Cell Res Ther. 2025 Aug 27;16(1):462. [Abstract]
- PLoS Biol. 2024 Jun 21;22(6):e3002666. [Abstract]
- Clin Transl Med. 2021 Jun;11(6):e467. [Abstract]
- Oncoimmunology. 2025 Dec;14(1):2460281. [Abstract]
- Fundam Res. 2024 Oct 18.
- J Agric Food Chem. 2025 Dec 10;73(49):31325-31335. [Abstract]
- Cell Mol Life Sci. 2024 Jul 30;81(1):320. [Abstract]
- Cell Mol Life Sci. 2019 Apr;76(8):1579-1593. [Abstract]
- Front Immunol. 2021 Mar 29;12:630380. [Abstract]
- Biochem Pharmacol. 2024 Jan:219:115939. [Abstract]
- J Ethnopharmacol. 2023 May 23:308:116271. [Abstract]
- Cancer Metab. 2026 Apr 15;14(1):15. [Abstract]
- Immunology. 2023 Jul;169(3):271-291. [Abstract]
- Int Immunopharmacol. 2026 Jul 1:180:116676. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2025 Mar 31;1871(5):167814. [Abstract]
- iScience. 2025 Sep 23;28(10):113631. [Abstract]
- PNAS Nexus. 2023 Feb 3;2(3):pgad038. [Abstract]
- J Virol. 2022 Feb 23;96(4):e0191921. [Abstract]
- Am J Pathol. 2024 Jul;194(7):1248-1261. [Abstract]
- Neuroscience. 2025 Dec 17:594:151-161. [Abstract]
- bioRxiv. 2026 Mar 10.
- SSRN. 2025 Dec 2.
- Res Sq 2025 Oct 1.
- bioRxiv. 2025 Sep 1.
- University of Padua. 2025.
- bioRxiv. 2025 May 23:2025.05.19.654627. [Abstract]
- bioRxiv. 2025 Feb 5:2025.01.30.635486. [Abstract]
- bioRxiv. 2024 August 17.
- SSRN. 2023 Nov 13.
- Research Square Preprint. 2023 Jul 18.
- Oxid Med Cell Longev. 2021 Jun 27;2021:5549047. [Abstract]
-
Flow Cytometry
-
Cell Imaging/Staining
-
WB
-
Cell Proliferation/Viability Assay
-
Bio/Physico-chemical Assay
Biologische Aktivität
IC50: 2.6 nM (hLDHA), 43 nM (hLDHB)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A673 | IC50 |
>57 μM
Compound: 2; GSK 2837808A
|
Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human A673 cells after 48 hrs by CellTiter-Glo assay
|
[PMID: 29120638] |
| A673 | IC50 |
0.84 μM
Compound: 2; GSK 2837808A
|
Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis
Cytotoxicity against human A673 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis
|
[PMID: 29120638] |
| MIA PaCa-2 | IC50 |
1.37 μM
Compound: 2; GSK 2837808A
|
Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis
Cytotoxicity against human MIAPaCa2 cells assessed as long term cell growth inhibition measured every 4 hrs for 120 hrs by incucyte zoom live cell analysis
|
[PMID: 29120638] |
| MIA PaCa-2 | IC50 |
28.4 μM
Compound: 2; GSK 2837808A
|
Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human MIAPaCa2 cells after 48 hrs by CellTiter-Glo assay
|
[PMID: 29120638] |
GSK2837808A rapidly and profoundly inhibits lactate production rates in multiple cancer cell lines including hepatocellular and breast carcinomas. The potency of GSK2837808A across 30 cancer cell lines with different LDHA and LDHB expression levels ranges from 400 nM to no effect (EC50 reported as 30 μM). GSK2837808A potency does not correlate with LDHA, LDHB, or the total LDH expression levels. GSK2837808A inhibits lactate production in hypoxia but at higher concentrations than in normoxia (EC50=10 μM). It also reduces ECAR with EC50=10 μM. LDH inhibition by GSK2837808A alters multiple metabolic pathways in Snu398 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS. Nr. 1445879-21-9
-
Appearance Solid
-
Molecular Weight 649.62
-
Formel C31H25F2N5O7S
-
Color Light yellow to yellow
-
SMILES
O=C(O)C1=CC(OC2=CC(F)=CC(F)=C2)=CC(NC3=C(S(=O)(NC4CC4)=O)C=NC5=CC(C6=CN=C(OC)N=C6OC)=CC=C35)=C1
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (47)
-
Journal Impact Factor
-
Most Recent
-
Mol Cancer
ROCK1 inhibition primes anti-tumor immunity in EGFR-mutant NSCLC by triggering PD-L1 degradation mediated by SMURF2. [Abstract]2026 Apr 2;25(1):130. PMID: 41928228 -
Cell Metab
2025 Apr 1;37(4):903-919.e10. PMID: 39933514
GSK2837808A purchased from MedChemExpress. Usage Cited in: Cell Metab. 2025 Apr 1;37(4):903-919.e10. [Abstract]
FACS quantification of STAR-based CSC percentage in TPO3 and TPO4 treated with LDHA inhibitor GSK2837808A (GSK, 100 µM, 3 days).
-
Gastroenterology
2024 Jan 24:S0016-5085(24)00064-7. PMID: 38272100
GSK2837808A purchased from MedChemExpress. Usage Cited in: Gastroenterology. 2024 Jan 24:S0016-5085(24)00064-7. [Abstract]
Phase-contrast images of dysplastic organoids treated with dimethyl sulfoxide (DMSO; vehicle), GSK2837808A (LDH inhibitor; 10 μM), 6-aminonicotinamide (G6PD inhibitor; 50 μM), telaglenastat (GLS1 inhibitor; 1 μM) for 3 days.
-
Nat Commun
LDHA-mediated ROS generation in chondrocytes is a potential therapeutic target for osteoarthritis. [Abstract]2020 Jul 9;11(1):3427. PMID: 32647171
GSK2837808A purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Jul 9;11(1):3427. [Abstract]
Chondrocytes were treated with IL-1β (10 ng/mL) in the presence of GSK2837808A (10 μM), oxamate (10 mM) or FX11 (40 μM) for 24 hours for supernatant lactic acid measurement.
-
Nat Commun
Interactome analysis reveals that lncRNA HULC promotes aerobic glycolysis through LDHA and PKM2. [Abstract]2020 Jun 22;11(1):3162. PMID: 32572027
GSK2837808A purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Jun 22;11(1):3162. [Abstract]
Proliferation of HepG2 cells with HULC knockdown (left panel) or overexpression (right panel) was measured with a CCK8 assay. For rescue experiments, HepG2-HULC cells were treated by FGFR1 inhibitor PD 166866 (2.5 μM), PKM2 activator DASA-58 (30 μM), or LDHA inhibitor GSK2837808A (10 μM), respectively.
-
Nat Commun
2019 Jun 20;10(1):2701. PMID: 31221965 -
Adv Sci (Weinh)
An Ultrasensitive Biosensor for Probing Subcellular Distribution and Mitochondrial Transport of l-2-Hydroxyglutarate. [Abstract]2024 Jul 15:e2404119. PMID: 39005231 -
J Adv Res
2025 Sep 26:S2090-1232(25)00756-8. PMID: 41016592 -
J Exp Clin Cancer Res
The IRF2/CENP-N/AKT signaling axis promotes proliferation, cell cycling and apoptosis resistance in nasopharyngeal carcinoma cells by increasing aerobic glycolysis. [Abstract]2021 Dec 10;40(1):390. PMID: 34893086 -
Cell Death Dis
PEBP4 alleviates muscle wasting in lung cancer cachexia via KEAP1-NRF2-mediated redox homeostasis. [Abstract]2026 Jun 3. PMID: 42236665 -
Cell Death Dis
Targeting LINC01711 in FAP+ cancer-associated fibroblasts overcomes lactate-mediated immunosuppression and enhances anti-PD-1 efficacy in lung adenocarcinoma. [Abstract]2025 Aug 25;16(1):642. PMID: 40855046 -
Int J Biol Macromol
Cepharanthine inhibits African swine fever virus replication by suppressing AKT-associated pathways through disrupting Hsp90-Cdc37 complex. [Abstract]2024 Oct 30:137070. PMID: 39486740 -
Int J Biol Macromol
Chicken muscle antibody array reveals the regulations of LDHA on myoblast differentiation through energy metabolism. [Abstract]2024 Jan;254(Pt 1):127629. PMID: 37890747 -
Acta Pharmacol Sin
Targeting PPARα activation sensitizes glioblastoma cells to temozolomide and reverses acquired resistance by inhibiting H3K18 lactylation. [Abstract]2025 Jun 11. PMID: 40500345 -
-
J Transl Med
Metabolic interplay between endometrial cancer and tumor-associated macrophages: lactate-induced M2 polarization enhances tumor progression. [Abstract]2025 Aug 18;23(1):923. PMID: 40826409 -
Stem Cell Res Ther
Extracellular lactate improves neurogenesis by modulating H3K9 lactylation and SnoN expression under hypoxic conditions. [Abstract]2025 Aug 27;16(1):462. PMID: 40866997 -
PLoS Biol
KCNK1 promotes proliferation and metastasis of breast cancer cells by activating lactate dehydrogenase A (LDHA) and up-regulating H3K18 lactylation. [Abstract]2024 Jun 21;22(6):e3002666. PMID: 38905316 -
Clin Transl Med
Functional inhibition of lactate dehydrogenase suppresses pancreatic adenocarcinoma progression. [Abstract]2021 Jun;11(6):e467. PMID: 34185423 -
Oncoimmunology
Leptin decreases Th17/Treg ratio to facilitate neuroblastoma via inhibiting long-chain fatty acid catabolism in tumor cells. [Abstract]2025 Dec;14(1):2460281. PMID: 39902867 -
-
J Agric Food Chem
Reducing Endogenous Lactate Production Ameliorates Ovalbumin-Induced Food Allergy via Regulating Lactylation and Microbial Homeostasis in Mice. [Abstract]2025 Dec 10;73(49):31325-31335. PMID: 41317116 -
Cell Mol Life Sci
Pharmacological induction of the hypoxia response pathway in Huh7 hepatoma cells limits proliferation but increases resilience under metabolic stress. [Abstract]2024 Jul 30;81(1):320. PMID: 39078527 -
Cell Mol Life Sci
Impairment of CFTR activity in cultured epithelial cells upregulates the expression and activity of LDH resulting in lactic acid hypersecretion. [Abstract]2019 Apr;76(8):1579-1593. PMID: 30599064 -
Front Immunol
2021 Mar 29;12:630380. PMID: 33854503 -
Biochem Pharmacol
Carfilzomib suppressed LDHA-mediated metabolic reprogramming by targeting ATF3 in esophageal squamous cell carcinoma. [Abstract]2024 Jan:219:115939. PMID: 38000560 -
J Ethnopharmacol
Shen Shuai II Recipe inhibits hypoxia-induced glycolysis by preserving mitochondrial dynamics to attenuate kidney fibrosis. [Abstract]2023 May 23:308:116271. PMID: 36806483
GSK2837808A purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2023 May 23:308:116271. [Abstract]
The conditioned media (CM) from hypoxia-treated NRK-52 E cells reduce the expression of FN, COL-Ⅰ, α-SMA and PCNA proteins in NRK-49 F cells after SSR (Shen Shuai II Recipe) and (or) GSK (GSK2837808A) treatment.
-
Cancer Metab
PFKFB4 promotes M2 polarization of tumor-associated macrophages through aerobic glycolysis-mediated modification of histone H3K18 lactylation in hepatocellular carcinoma. [Abstract]2026 Apr 15;14(1):15. PMID: 41987314 -
Immunology
Inactivation of mitochondrial pyruvate carrier promotes NLRP3 inflammasome activation and gout development via metabolic reprogramming. [Abstract]2023 Jul;169(3):271-291. PMID: 36708143 -
Int Immunopharmacol
Triptolide alleviates rheumatoid arthritis by inhibiting lactate-mediated activation of mTORC1/HIF-1α to restrain Th17 cell differentiation. [Abstract]2026 Jul 1:180:116676. PMID: 42013646 -
Biochim Biophys Acta Mol Basis Dis
Triiodothyronine promotes the proliferation and chemoresistance of cholangiocarcinoma cells via HIF-1α/Glut1-stimulated glycolysis. [Abstract]2025 Mar 31;1871(5):167814. PMID: 40168755 -
iScience
2025 Sep 23;28(10):113631. PMID: 41126894 -
PNAS Nexus
The function of lactate dehydrogenase A in retinal neurons: implications to retinal degenerative diseases. [Abstract]2023 Feb 3;2(3):pgad038. PMID: 36896135 -
J Virol
African Swine Fever Virus Regulates Host Energy and Amino Acid Metabolism To Promote Viral Replication. [Abstract]2022 Feb 23;96(4):e0191921. PMID: 34908441 -
Am J Pathol
Differentiation of Type 17 Mucosal-Associated Invariant T Cells in Circulation Contributes to the Severity of Sepsis. [Abstract]2024 Jul;194(7):1248-1261. PMID: 38599461 -
Neuroscience
Tongqiao Huoxue Decoction modulates glycolysis and activates the BDNF-TrkB pathway by lactate to protect PC12 cells from OGD-induced injury. [Abstract]2025 Dec 17:594:151-161. PMID: 41418872 -
-
-
-
-
-
bioRxiv
3D Endothelium-on-a-Chip Reveals Cx43/LDHA Axis as a Driver of Endothelial Barrier Dysfunction in Diabetic Kidney Disease. [Abstract]2025 May 23:2025.05.19.654627. PMID: 40475678 -
bioRxiv
Hypoxia-induced histone methylation and NF-κB activation in pancreas cancer fibroblasts promote EMT-supportive growth factor secretion. [Abstract]2025 Feb 5:2025.01.30.635486. PMID: 39974981 -
-
-
-
Oxid Med Cell Longev
NOX4-Derived ROS Mediates TGF- β 1-Induced Metabolic Reprogramming during Epithelial-Mesenchymal Transition through the PI3K/AKT/HIF-1 α Pathway in Glioblastoma. [Abstract]2021 Jun 27;2021:5549047. PMID: 34257808
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (76.97 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.5 mg/mL (3.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Protokoll
Sixty thousand Snu398 cells per well are plated in 6-well tissue culture plates in RPMI-1640 medium supplemented with 2.5% charcoal-stripped FBS. Cells are allowed to attach overnight and then DMSO control or the indicated doses of LDHA inhibitor dissolved in DMSO are added directly to the wells. After 4 to 8 days of incubation in the indicated oxygen conditions, adherent cells are trypsinized, counted, and had their viability assessed by the trypan-blue exclusion method using the Vi-Cell XR Cell Viability Analyzer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: GSK2837808A is administered to male CD mice or male Sprague-Dawley rats orally or by intravenous (IV) infusion over 120 minutes into a femoral vein. Arterial blood samples are collected over time and GSK2837808A concentration is determined by liquid chromatography (LC)/MS/MS analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
-
Data Sheet (281 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
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 | 1.5394 mL | 7.6968 mL | 15.3936 mL | 38.4840 mL |
| 5 mM | 0.3079 mL | 1.5394 mL | 3.0787 mL | 7.6968 mL | |
| 10 mM | 0.1539 mL | 0.7697 mL | 1.5394 mL | 3.8484 mL | |
| 15 mM | 0.1026 mL | 0.5131 mL | 1.0262 mL | 2.5656 mL | |
| 20 mM | 0.0770 mL | 0.3848 mL | 0.7697 mL | 1.9242 mL | |
| 25 mM | 0.0616 mL | 0.3079 mL | 0.6157 mL | 1.5394 mL | |
| 30 mM | 0.0513 mL | 0.2566 mL | 0.5131 mL | 1.2828 mL | |
| 40 mM | 0.0385 mL | 0.1924 mL | 0.3848 mL | 0.9621 mL | |
| 50 mM | 0.0308 mL | 0.1539 mL | 0.3079 mL | 0.7697 mL | |
| 60 mM | 0.0257 mL | 0.1283 mL | 0.2566 mL | 0.6414 mL |