(R)-GNE-140

Research use only, not for human use.

(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.

(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.

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GNE-140 | GNE 140 | GNE140

Metabolic Enzyme/Protease

LDH

LDH

Cancer

Pancreatic Cancer

2003234-63-5

499.0447

C25H23ClN2O3S2

>98% (HPLC)

10 mM in DMSO

C1COCCN1C2=CC=C(C=C2)C3(CC(=C(C(=O)N3)SC4=CC=CC=C4Cl)O)C5=CSC=C5

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(-20℃)

With Ice Pack

≥ 2 years