Sigma Aldrich Fine Chemicals Biosciences GLS1 Inhibitor III CB-839

Supplier:  Sigma Aldrich Fine Chemicals Biosciences 5337170001

A cell-permeable orally available thiadiazolyl-butyl-pyridazinyl compound that acts as a potent selective time-dependent and slowly-reversible (t1/2 45 min at 25 C) inhibitor of glutaminase (IC50 45 23 and 28 nM for rec hu-GAC KGA and GAC respectively). The inhibition appears to be non-competitive and allosteric. Exhibits anti-proliferative effects in HCC1806 and MDA-MB-231 triple-negative breast cancer cell lines (IC50 49 and 26 nM respectively) but does not affect the viability of ER/HER2-T47D cell line. Shown to reduce glutamine consumption (IC50 17 nM) and glutamate production (IC50 15 nM) rates in HCC1806 cells. Inhibits the growth of HCC1806 xenografts in mice (~200 mg/kg p.o. b.i.d) and of JIMT-1 xenografts (200 mg/kg p.o. b.i.d) either alone or in combination with paclitaxel (10 mg/kg 5 doses alternate days).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certifica

Catalog No. 50-289-7381