DC Chemicals · Product datasheet

(R)-GNE-140 — Datasheet

CAT. NO. DC23181

Product page and current package options

ParameterValue
Chemical NameR-GNE-140
CAS No.2003234-63-5
Synonyms(R)-GNE-140;(R)-3-((2-chlorophenyl)thio)-4-hydroxy-6-(4-morpholinophenyl)-6-(thiophen-3-yl)-5,6-dihydropyridin-2(1H)-one;(2~{r})-5-(2-Chlorophenyl)sulfanyl-2-(4-Morpholin-4-Ylphenyl)-4-Oxidanyl-2-Thiophen-3-Yl-1,3-Dihydropyridin-6-One;BDBM197160;s6675;AK00798569;J3.623.769D;Q27460797
FormulaC25H23ClN2O3S2
M.Wt499.04
SMILESClC1=C([H])C([H])=C([H])C([H])=C1SC1C(N([H])[C@@](C2=C([H])SC([H])=C2[H])(C2C([H])=C([H])C(=C([H])C=2[H])N2C([H])([H])C([H])([H])OC([H])([H])C2([H])[H])C([H])([H])C=1O[H])=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

(R)-GNE-140 (GNE-140) is a novel potent, selective lactate dehydrogenase (LDH) inhibitor with IC50 of 3, 5, and 5 nM for LDHA, LDHB, and LDHC, respectively; displays no inhibition on malate MDH-1, MDH-2 (IC50>10 uM for both enzymes), and no appreciable inhibition against a panel of 301 kinases (<50% inhibition at 1 uM); perturbs glycolysis and inhibits proliferation in MIA PaCa-2 cells (IC50=0.43 uM), decreases glucose uptake (IC50=0.47 uM); pancreatic cell lines that utilize oxidative OXPHOS rather than glycolysis are inherently resistant to GNE-140, which can be resensitized to GNE-140 with the OXPHOS inhibitor phenformin.

Pancreatic Cancer

Phase 1 Clinical

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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