Name | BPTES |
Synonyms | BPTES CS-1542 Glutaminase Inhibitor II Glutaminase Inhibitor II, BPTES bis-2-(5-phenylaQtMido-1,2,4-Thiadiazol-2-yl)Ethylsulfide bis-2-(5-PhenylacetMido-1,2,4-Thiadiazol-2-yl)Ethyl Sulfide Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide N,N'-[Thiobis(2,1-ethanediyl-1,3,4-thiadiazole-5,2-diyl)]bisbenzeneacetamide |
CAS | 314045-39-1 |
Molecular Formula | C24H24N6O2S3 |
Molar Mass | 524.68 |
Density | 1.420±0.06 g/cm3(Predicted) |
Solubility | DMSO: 52 mg/mL (Need ultrasonic and warming) |
Appearance | powder |
Color | white to beige |
pKa | 9.13±0.50(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
In vitro study | BPTES inhibited glutaminase with an IC50 of 0.18 μm in human kidney cells and glutamate by microglia with an IC50 of 80-120 nM. In D54 cells containing mutant IDH1, BPTES preferentially slowed their cell growth. BPTES also inhibited glutaminase activity, decreased glutamate and α-kg levels, and increased glycolytic intermediates. BPTES (10 μm) inhibited the growth of mHCC 3-4 cells derived from LAP/MYC tumors. BPTES also inhibits the growth of MYC-dependent P493 cells by blocking DNA replication, causing cell death and lysis. |
In vivo study | In LAP/MYC mice, BPTES (12.5 mg/kg, I. p.) prolonged survival without significant effects on MYC,GLS, or GLS2 levels. In mice bearing P493 tumor xenografts, BPTES (200 μg/mouse, I. p.) also inhibited tumor cell growth. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.906 ml | 9.53 ml | 19.059 ml |
5 mM | 0.381 ml | 1.906 ml | 3.812 ml |
10 mM | 0.191 ml | 0.953 ml | 1.906 ml |
5 mM | 0.038 ml | 0.191 ml | 0.381 ml |
biological activity | BPTES is a potent and selective glutamine GLS1 (KGA) inhibitor with an IC50 of 0.16 μm. It has no effect on the activity of glutamate dehydrogenase, and has only a weak inhibitory effect on the activity of gamma glutamyl transpeptidase. |
Target | Value |
Glutaminase GLS1 (KGA) | 0.16 μM |