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Chemical Structure| 1445879-21-9 Chemical Structure| 1445879-21-9

Structure of GSK2837808A
CAS No.: 1445879-21-9

Chemical Structure| 1445879-21-9

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GSK2837808A is a potent and selective LDHA and LDHB inhibitor with IC50 values of 2.6nM and 43nM for LDHA and LDHB, respectively. It reduces glucose uptake and enhances mitochondrial oxygen consumption in Snu398 hepatocellular carcinoma cells.

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Product Details of GSK2837808A

CAS No. :1445879-21-9
Formula : C31H25F2N5O7S
M.W : 649.62
SMILES Code : 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
MDL No. :MFCD28133406
InChI Key :RZBCPMYJIARMGV-UHFFFAOYSA-N
Pubchem ID :71533725

Safety of GSK2837808A

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2 cells 75 μM 24 hours Decreased the level of TPX2 lactylation Life Sci Alliance. 2025 Mar 19;8(6):e202402978
nasopharyngeal carcinoma cells 10 μmol/L GSK2837808A blocked the promotion of aerobic glycolysis in NPC cells induced by overexpression of CENP-N J Exp Clin Cancer Res. 2021 Dec 10;40(1):390
THP-1-derived macrophages 10 μM 45 minutes GSK2837808A inhibited nigericin-induced IL-1β secretion Front Immunol. 2021 Mar 29;12:630380
cardiomyocytes 10 μM inhibited LDHA activity, reduced lactate accumulation, and improved insulin signaling Biol Direct. 2023 Sep 4;18(1):54
BV2 microglia 100 μM 20 hours (for NAD+/NADH assay) or 23.5 hours (for NO, iNOS, and COX2 assays) GSK2837808A completely reversed the effects of pyruvate on the cytosolic NAD+/NADH ratio in LPS-stimulated BV2 microglia treated with AOAA and significantly attenuated the restorative effects of pyruvate on iNOS and COX2 protein levels Front Mol Biosci. 2021 Jul 26;8:655687
HeLa cells 75 µM 24 hours To evaluate the inhibitory effect of GSK2837808A on lactate dehydrogenase activity in HeLa cells, results showed that GSK2837808A significantly inhibited lactate production. Cancer Metab. 2018 Dec 12;6:19
U2OS cells 40 μM 24 hours Evaluate the effect of GSK2837808A in combination with Chk1 inhibitor on DNA damage, showing that 40 μM GSK combined with Chk1i reduced cell viability by 2.1-fold in U2OS cells. Sci Rep. 2017 Jan 20;7:40778
HT29 cells 40 μM 24 hours Evaluate the effect of GSK2837808A in combination with Chk1 inhibitor on DNA damage, showing that 40 μM GSK combined with Chk1i reduced cell viability by 2.1-fold in U2OS cells. Sci Rep. 2017 Jan 20;7:40778

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Orthotopic pancreatic cancer model Oral 6 mg/kg/QD Once daily for 4 weeks To evaluate the effect of LDH inhibitor on tumor growth and immune microenvironment Cancer Res. 2021 Aug 1;81(15):4001-4013
C57BL/6J mice MSU-induced peritonitis model Intraperitoneal injection 20 mg/kg Single dose, lasting 4 hours GSK2837808A reduced IL-1β production and neutrophil recruitment in MSU-induced peritonitis Front Immunol. 2021 Mar 29;12:630380
Nude mice HCC xenograft model Intraperitoneal injection 6 mg/kg Every 3 days Suppressed tumor growth Life Sci Alliance. 2025 Mar 19;8(6):e202402978

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.54mL

0.31mL

0.15mL

7.70mL

1.54mL

0.77mL

15.39mL

3.08mL

1.54mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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