GNE-140 racemate| CAS 1802977-61-2

Cas No.:	1802977-61-2
Chemical Name:	GNE-140 (racemate)
Synonyms:	GNE-140 (racemate);GNE 140 racemate;BDBM50103567;SB18723;3-((2-chlorophenyl)thio)-6-(4-morpholinophenyl)-6-(thiophen-3-yl)piperidine-2,4-dione;ClC1=C(C=CC=C1)SC1C(NC(CC1=O)(C1=CSC=C1)C1=CC=C(C=C1)N1CCOCC1)=O;3-[(2-chlorophenyl)sulfanyl]-6-[4-(morpholin-4-yl)phenyl]-6-(thiophen-3-yl)piperidine-2,4-dione;GNE-140 racemate
SMILES:	ClC1=C([H])C([H])=C([H])C([H])=C1SC1([H])C(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])C1=O)=O
Formula:	C₂₅H₂₃ClN₂O₃S₂
M.Wt:	499.0447
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

The racemate of GNE-140, 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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