For research use only. Not for therapeutic Use.
R-GNE-140 is a potent inhibitor of LDHA and LDHB enzymes, exhibiting selective inhibition with IC50 values of 3 nM and 5 nM, respectively. In comparison to its S-isomer, it is 18 times more potent. The compound’s selectivity and potency make it a promising candidate for use in cancer therapy and metabolic disorders, where LDHA and LDHB have been implicated in disease progression.
| Catalog Number | I014663 |
| CAS Number | 2003234-63-5 (R-isomer) |
| Synonyms | R-GNE-140; (R)-GNE-140; GNE 140; GNE140.;(R)-3-((2-Chlorophenyl)thio)-4-hydroxy-6-(4-morpholinophenyl)-6-(thiophen-3-yl)-5,6-dihydropyridin-2(1H)-one |
| Molecular Formula | C25H23ClN2O3S2 |
| Purity | ≥95% |
| Target | Lactate Dehydrogenase |
| Solubility | Soluble in DMSO |
| Storage | 2-8°C(protect from light) |
| IUPAC Name | (2R)-5-(2-chlorophenyl)sulfanyl-4-hydroxy-2-(4-morpholin-4-ylphenyl)-2-thiophen-3-yl-1,3-dihydropyridin-6-one |
| InChI | InChI=1S/C25H23ClN2O3S2/c26-20-3-1-2-4-22(20)33-23-21(29)15-25(27-24(23)30,18-9-14-32-16-18)17-5-7-19(8-6-17)28-10-12-31-13-11-28/h1-9,14,16,29H,10-13,15H2,(H,27,30)/t25-/m1/s1 |
| InChIKey | SUFXXEIVBZJOAP-RUZDIDTESA-N |
| SMILES | C1COCCN1C2=CC=C(C=C2)C3(CC(=C(C(=O)N3)SC4=CC=CC=C4Cl)O)C5=CSC=C5 |
| Reference | </br>1: Boudreau A, Purkey HE, Hitz A, Robarge K, Peterson D, Labadie S, Kwong M, Hong</br> R, Gao M, Del Nagro C, Pusapati R, Ma S, Salphati L, Pang J, Zhou A, Lai T, Li Y,</br> Chen Z, Wei B, Yen I, Sideris S, McCleland M, Firestein R, Corson L, Vanderbilt</br> A, Williams S, Daemen A, Belvin M, Eigenbrot C, Jackson PK, Malek S,</br> Hatzivassiliou G, Sampath D, Evangelista M, O’Brien T. Metabolic plasticity</br> underpins innate and acquired resistance to LDHA inhibition. Nat Chem Biol. 2016 </br> Oct;12(10):779-86. doi: 10.1038/nchembio.2143. Epub 2016 Aug 1. PubMed PMID:</br> 27479743.</br> </br> |
