GNE-140 racemate free base

GNE-140 racemate is a racemic mixture of (R)-GNE-140 and (S)-GNE-140 , and also a tautomer of GNE-140 .

For research use only. Not for human or veterinary use.

Target Lactate Dehydrogenase p38 MAPK EGFR Akt Caspase Reactive Oxygen Species (ROS)

Research area Inflammation/Immunology Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GNE-140 racemate structure

CAS No.: 1802977-61-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 498.00	BP-02523-25mg	In stock	Get quote
50 mg	USD 698.00	BP-02523-50mg	In stock	Get quote
100 mg	USD 985.00	BP-02523-100mg	In stock	Get quote
250 mg	USD 1,685.00	BP-02523-250mg	In stock	Get quote
500 mg	Inquire	BP-02523-500mg	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

GNE-140 racemate is a racemic mixture of (R)-GNE-140 and (S)-GNE-140 , and also a tautomer of GNE-140 . GNE-140 racemate is an orally active lactate dehydrogenase inhibitor, with an IC50 of 3 nM against human LDHA and an IC50 of 5 nM against LDHB. GNE-140 racemate reduces the phosphorylation level and total protein expression of p38 MAPK, and inhibits EGF-induced AKT phosphorylation. GNE-140 racemate decreases lactate production, regulates glycolysis, the pentose phosphate pathway and nucleotide biosynthesis, increases extracellular pH, inhibits cell proliferation, migration and invasion, and induces caspase-3 activation and ROS accumulation. GNE-140 racemate can be used in research related to breast cancer, cystic fibrosis and pancreatic cancer .

Biological activity

GNE-140 racemate is a racemic mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is also a potent lactate dehydrogenase A (LDHA) inhibitor.

Identifiers

SMILES: C1COCCN1C2=CC=C(C=C2)C3(CC(=O)C(C(=O)N3)SC4=CC=CC=C4Cl)C5=CSC=C5
InChIKey: GLDDJXYFHWRGPI-UHFFFAOYSA-N

Specifications

MW (average): 499.0450
Formula: C₂₅H₂₃ClN₂O₃S₂
CAS No.: 1802977-61-2
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO

In vitro: DMSO : 20 mg/mL

Documents

References

[1].Khajah MA, et al. The effect of lactate dehydrogenase inhibitors on proliferation, motility and invasion of breast cancer cells highlights a new role for lactate. Molecular medicine reports. 2024 Jan;29(1):12.

[2].Valdivieso ÁG, et al. Impairment of CFTR activity in cultured epithelial cells upregulates the expression and activity of LDH resulting in lactic acid hypersecretion. Cellular and molecular life sciences : CMLS. 2019 Apr;76(8):1579-1593.

[3].Boudreau A, et al. Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition. Nature chemical biology. 2016 Oct;12(10):779-86.

[4].Ji JJ, et al. Kallistatin/Serpina3c inhibits cardiac fibrosis after myocardial infarction by regulating glycolysis via Nr4a1 activation. Biochimica et biophysica acta. Molecular basis of disease. 2022 Sep 01;1868(9):166441.

Same target

Search Lactate Dehydrogenase

Same research area

Search Inflammation/Immunology