GNE-140 racemate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GNE-140 的外消旋体，一种新型有效的选择性乳酸脱氢酶 (LDH) 抑制剂，对 LDHA、LDHB 和 LDHC 的 IC50 值分别为 3、5 和 5 nM。

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.

——

——

GNE 140 racemate | GNE140 racemate

Metabolic Enzyme/Protease

LDH

LDH

Cancer

Pancreatic Cancer

1802977-61-2

499.0447

C25H23ClN2O3S2

>98% (HPLC)

DMSO: ≥ 34 mg/mL

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

2,4-Piperidinedione, 3-[(2-chlorophenyl)thio]-6-[4-(4-morpholinyl)phenyl]-6-(3-thienyl)-

(-20℃)

With Ice Pack

≥ 2 years