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Chemical Structure| 2003234-63-5 Chemical Structure| 2003234-63-5

Structure of (R)-GNE-140
CAS No.: 2003234-63-5

Chemical Structure| 2003234-63-5

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(R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor with IC50s of 3 nM and 5 nM for LDHA and LDHB respectively.

Synonyms: (R)-GNE-140

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Product Details of (R)-GNE-140

CAS No. :2003234-63-5
Formula : C25H23ClN2O3S2
M.W : 499.04
SMILES Code : O=C1N[C@@](C2=CSC=C2)(C3=CC=C(N4CCOCC4)C=C3)CC(O)=C1SC5=CC=CC=C5Cl
Synonyms :
(R)-GNE-140
MDL No. :MFCD31560470
InChI Key :SUFXXEIVBZJOAP-RUZDIDTESA-N
Pubchem ID :121225870

Safety of (R)-GNE-140

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Th17 cells 10 μM 3 days GNE-140 could decrease the percentage of IL-17+CD4 T cells, suggesting the suppressor role of GNE-140 on Th17 differentiation in Bcl-3-/- mice PMC9500237
rat alveolar bone marrow mesenchymal cells (ABMMCs) 10 μM 24 h Inhibited lactate dehydrogenase A (LDHA) activity, reduced lactate production, thereby suppressing osteogenic differentiation, proliferation, and migration of ABMMCs, and promoting apoptosis PMC9738738
MDA-MB-231 cells 50 μM 24 h to 7 days To evaluate the effects of GNE-140 on lactic acid production, glucose utilization, cell viability, and mitochondrial membrane potential in MDA-MB-231 cells. Results showed that GNE-140 fully blocked lactic acid production, inhibited glucose utilization and the glycolytic pathway, but had no adverse effects on cell viability or mitochondrial membrane potential, only attenuating cell division. PMC8698706
mouse melanoma B16-F10 cells 10 μM 1 h inhibited LDHA and LDHB activity, mimicking the metabolic phenotype of LDHA/B-DKO cells, characterized by suppressed glycolysis and reactivated OXPHOS PMC6187639
human colon adenocarcinoma LS174T 10 μM 1 h inhibited LDHA and LDHB activity, mimicking the metabolic phenotype of LDHA/B-DKO cells, characterized by suppressed glycolysis and reactivated OXPHOS PMC6187639

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.00mL

0.40mL

0.20mL

10.02mL

2.00mL

1.00mL

20.04mL

4.01mL

2.00mL

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
Protocol 2

References

 

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