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Description: BPTES is a potent and selective allosteric Glutaminase GLS1 (KGA) inhibitor with IC50 of 0.16 uM. BPTES inhibits glutaminase activity expressed in human kidney cells with IC50 of 0.18 uM, and inhibits glutamate efflux by microglia with IC50 of 80-120 nM. BPTES preferentially slows cell growth in D54 cells with mutant IDH1. BPTES also inhibits glutaminase activity, lowers glutamate and alpha-KG levels, and increases glycolytic intermediates. BPTES (10 uM) inhibits cell growth of mHCC 3–4 cells derived from LAP/MYC tumors. BPTES also inhibits growth of a MYC-dependent P493 cells by blocking DNA replication, leading to cell death and fragmentation.
References: Cancer Res. 2010 Nov 15; 70(22):8981-7; J Clin Invest. 2015 Jun; 125(6):2293-306.
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