(R)-GNE-140

Catalog No.S6675 Batch:S667501

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Technical Data

Formula

C25H23ClN2O3S2
Molecular Weight 499.04 CAS No. 2003234-63-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (200.38 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description (R)-GNE-140 is a selective inhibitor of the LDHA and LDHB with IC50s of 3 nM and 5 nM, respectively. The R enantiomer of GNE-140 is 18-fold more potent than S enantiomer.
Targets
LDHA [1]
(Cell-free assay)		 LDHB [1]
(Cell-free assay)
3 nM 5 nM
In vitro

(R)-GNE-140 inhibits proliferation in 37 of 347 cancer cell lines tested at a potency cut off of 5 μM. (R)-GNE-140 exhibits inhibition with two chondrosarcoma (bone) cancer cell lines that harbored IDH1 mutations (IC50 = 0.8μM).(R)-GNE-140 has submicromolar MiaPaca2 potency and inhibits proliferation in 11% of cancer cell lines in a broad panel. [1]
In vivo

(R)-GNE-140 presents a low Clp, and also had high bioavailability when dosed orally at 5 mg/kg to mice. At higher oral doses, ranging from 50 to 200 mg/kg, (R)-GNE-140 displays greater in vivo exposure.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    105KC,JJ012,143B,G84,1321N1,ONS-76,G22,G140,G96,HCC1143,CAL-120,Hs 578T,SISO,SKG-II,HCT-15,KYSE-520,KMRC-1,SNU-475,SNU-423,HT-1080,NCI-H1437,NCI-H1339,LXF-289,MCAS,PA-1,Hs 38.T,59M,MIA PaCa-2,SW 1990,PSN1,GR-M,Hs 746T,MKN-74,S-117,FTC-238,B-CPAP,HEC-265 cell lines

  • Concentrations

    6 pt dose titration scheme

  • Incubation Time

    72 h

  • Method

    Cells are plated using optimal seeding densities in 384-well plates using RPMI, 5% FBS, 100 ug/ml penicillin, 100 units/ml streptomycin. Optimal seeding densities are established for each cell line in order to reach 75-80% confluence at the end of the assay. The following day, cells are treated with (R)-GNE-140 using a 6 pt dose titration scheme. After 72 hours, cell viability is assessed using the CellTiter-Glo® Luminescence Cell Viability assay. Absolute inhibitory concentration (IC) values are calculated using four-parameter logistic curve fitting.
Animal Study:

[1]
  • Animal Models

    Female CD-1 mice

  • Dosages

    IV: 1.0 mg/kg; Oral: 5,50,100,200 mg/kg

  • Administration

    IV / Oral

Selleck's (R)-GNE-140 has been cited by 2 publications

Lactate promotes myogenesis via activating H3K9 lactylation-dependent up-regulation of Neu2 expression [ J Cachexia Sarcopenia Muscle, 2023, 10.1002/jcsm.13363] PubMed: 37919243
Host T cell dedifferentiation effects drive HIV-1 latency stability [ J Virol, 2022, jvi0197421] PubMed: 35019721

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.