| Description | BPTES(IC50 of 0.16 μM) is an effective and specific GlutamiN/Ase GLS1 (KGA) inhibitor. |
| In vitro | BI-9564 with EC50 of 800 nM.BRD7 implied as a tumor suppressor and is down-regulated in cancer cells, BI-9564 shows Kd of 73 nM for it, and is >10-fold more selective for BRD9 over the high homologues bromodomain. BI-9564 (40% is observed for only 2 out of 55 GPCRs. |
| In vivo | In LAP/MYC mice, BPTES (12.5 mg/kg, i.p.) prolongs survival with no significant effects on MYC, GLS, or GLS2 levels. BPTES (200 μg/mouse, i.p.) also inhibits tumor cell growth in mice harboring P493 tumor xenografts. [3] |
| Cell experiments | BPTES is dissolved in DMSO. Cells are plated at a density of 500 cells/well in a 96-well black clear bottom plate. At 24 hrs, media is changed to the appropriate media (DMEM with 4.5 g/L, 1.5 g/L or 0.1 g/L glucose, 10% FBS, pencillin/streptomycin, and 4 mM glutamine with or without doxycyline). 48 hours after plating, compounds or DMSO are added. Media and alamarBlue is added to a volume of 200 μL in each well. Fluorescence is measured at 48 hrs or 72 hrs (EGCG) using a Victor3 plate-reader. |
| Target activity | Glutaminase GLS1:0.16 μM |
| molecular weight | 524.68 |
| Molecular formula | C24H24N6O2S3 |
| CAS | 314045-39-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 10.5 mg/mL (20 mM) |
| References | 1. Newcomb R. 2002. U.S. Pat. 6,451,828 B1. 2. Seltzer MJ, et al. Cancer Res. 2010, 70(22), 8981-81987. 3. Xiang Y, et al. J Clin Invest. 2015, 125(6), 2293-2306. 6. Lee JS, et al. Dual targeting of glutaminase 1 and thymidylate synthase elicits death synergistically in NSCLC. Cell Death Dis. 2016 Dec 8;7(12):e2511. |
| Citations | 1. Qi J, Gao X, Zhong X, et al. Selective inhibition of Aurora A and B kinases effectively induces cell cycle arrest in t(8;21) acute myeloid leukemia. Biomedicine & Pharmacotherapy. 2019, 117: 109113. 2. Zhu B, Wei X, Narasimhan H, et al.Inhibition of the mitochondrial pyruvate carrier simultaneously mitigates hyperinflammation and hyperglycemia in COVID-19.Science immunology.2023: eadf0348. |