bs-7056C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 499.04

Formula: C25 H23 Cl N2 O3 S2

CAS Number: 2003234-63-5

InChi Key: SUFXXEIVBZJOAP-RUZDIDTESA-N

InChi: InChI=1S/C25H23ClN2O3S2/c26-20-3-1-2-4-22(20)33-23-21(29)15-25(27-24(23)30,18-9-14-32-16-18)17-5-7-19(8-6-17)28-10-12-31-13-11-28/h1-9,14,16,29H,10-13,15H2,(H,27,30)/t25-/m1/s1

Smiles: OC1C[C@](NC(=O)C=1SC1C=CC=CC=1Cl)(C1=CSC=C1)C1C=CC(=CC=1)N1CCOCC1

Purity: 98.0

Solubility: Soluble in DMSO

Appearance: Solid Power.

Shelf Life: 1.0 years

Description:

R-GNE-140 a novel potent lactate dehydrogenase (LDHA) inhibitor with IC50 3nM for LDHA and 5 nM for LDHB. In MIA PaCa-2 human pancreatic cells, LDHA inhibition rapidly affected global metabolism, although cell death only occurred after 2 d of continuous LDHA inhibition. Pancreatic cell lines that utilize oxidative phosphorylation (OXPHOS) rather than glycolysis were inherently resistant to GNE-140, but could be resensitized to GNE-140 with the OXPHOS inhibitor phenformin. Acquired resistance to GNE-140 was driven by activation of the AMPK-mTOR-S6K signaling pathway, which led to increased OXPHOS, and inhibitors targeting this pathway could prevent resistance.