(R)-GNE-140 是LDHA抑制剂，能够作用于 LDHA (IC50:3 nM) 和 LDHB (IC50:3 nM)。它的活性是 S 型异构体的 18 倍。

(R)-GNE-140 is an effective LDHA/LDHB inhibitor (IC50s: 3/5 nM) and is 18-fold more potent than S enantiomer.

(R)-GNE-140 (5 μM) inhibits proliferation in 37 of 347 cancer cell lines. (R)-GNE-140 has an inhibitory effect on two chondrosarcomas (bone) cancer cell lines that harbor IDH1 mutations (IC50: 0.8 mΜ).

(R)-GNE-140 (5 mg/kg) has high bioavailability in mice. (R)-GNE-140 (50-200 mg/kg, p.o.) has greater exposure.

2003234-63-5

C25H23ClN2O3S2

499.04

GNE-140;(R)-GNE-140

H2O:< 0.1 mg/mL (insoluble)
DMSO:14.43 mg/mL (28.92 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years