BPTES

Catalog No.S7753

For research use only.

BPTES is a potent and selective Glutaminase GLS1 (KGA) inhibitor with IC50 of 0.16 μM. It has no effect on glutamate dehydrogenase activity and causes only a very slight inhibition of γ-glutamyl transpeptidase activity.

BPTES Chemical Structure

CAS No. 314045-39-1

Selleck's BPTES has been cited by 33 publications

Purity & Quality Control

Choose Selective Glutaminase Inhibitors

Biological Activity

Description BPTES is a potent and selective Glutaminase GLS1 (KGA) inhibitor with IC50 of 0.16 μM. It has no effect on glutamate dehydrogenase activity and causes only a very slight inhibition of γ-glutamyl transpeptidase activity.
Targets
Glutaminase GLS1 (KGA) [1]
0.16 μM
In vitro

BPTES inhibits glutaminase activity expressed in human kidney cells with IC50 of 0.18 μM, and inhibits glutamate efflux by microglia with IC50 of 80-120 nM. [1] BPTES preferentially slows cell growth in D54 cells with mutant IDH1. BPTES also inhibits glutaminase activity, lowers glutamate and α-KG levels, and increases glycolytic intermediates. [2] BPTES (10 μM) 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. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 cell M3rNRWN6fG:2b4jpZ4l1gSCjc4PhfS=> MYS2JIRigXN? NFjKO3hEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJI1m[XO3cnXkJI9vKD[2aDDkZZkh[nliaHXtc4N6fG:vZYTyfUwhUUN3ME2yMlYyKM7:TR?= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjl6OEiwN{c,OjZ7OEi4NFM9N2F-
MDA-MB-231 M4fwTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVm3NkBpenN? MofsS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTTJIF{e2G7LDDJR|UxKD1iNj64JO69VS5? Mk\5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4MEmxNFEoRjJ6NkC5NVAyRC:jPh?=
Aspc-1 NXjVO|BZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVm3NkBpenN? NXX1bYd4T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hSXOyYz2xJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSBzMD6yJO69VS5? MnfFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4MEmxNFEoRjJ6NkC5NVAyRC:jPh?=
HCC827 Mli3R5l1d3SxeHnjbZR6KGG|c3H5 NF7DeI81QCCqcoO= M4HaOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJIVzdG:2aX7pZk1z\XOrc4ThcpQhUEOFOEK3JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyIE2gOFIvPCEQvF2u M{iyXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUe0NVA2Lz5{OEG3OFExPTxxYU6=
HT1080 NHjIWYNEgXSxdH;4bYNqfHliYYPzZZk> MkHiOFghcHK| NWHBeJJ1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRzMEiwJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IES4JIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyIE2gOFcvPzJizszNMi=> NVi0S3RORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixO|QyODVpPkK4NVc1OTB3PD;hQi=>
Assay
Methods Test Index PMID
Western blot γH2AX ; c-Myc / KLF4 / SOX2 / OCT4 / NANOG / GLS1 29107960 30555042
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]

Protocol (from reference)

Kinase Assay:

[1]

  • Glutaminase Inhibition: Cell Free Assay:

    Assay plates are prepared containing 2 μL test compound in DMSO/well. The enzyme is diluted to 1 unit (liver) or 0.8 unit (kidney)/100 μL in glutaminase assay buffer, and 100 μL diluted enzyme is added to each well of the assay plate by Multidrop. The contents are mixed by shaking at full speed for 1 min on TiterMix 100. The plates are preincubated at room temperature (RT) for 20 min to allow binding of test compounds to glutaminase, and 50 μL glutamine solution (7 mM in assay buffer) is added to each well by Multidrop. The contents are shaken at full speed for 30 sec on TiterMix 100, and the plates are then incubated at RT for 60 min (liver) or 90 min (kidney). To stop the reactions, 20 μL HCl (0.3 N) is added to each well by Multidrop and mixed immediately by shaking for 30 sec on TiterMix 100. For quantification, glutamate (formed by glutaminase-catalyzed hydrolysis of glutamine) is oxidized to 2-oxoglutarate by a second enzyme, glutamate dehydrogenase (GDH), with the concomitant production of the reduced form of nicotinamide adenine dinucleotide (NADH). Reduction of nitro blue tetrazolium (NBT) in the assay solution by NADH, catalyzed by phenazine methosulphate (PMS), results in the formation of a blue-purple formazan. The absorption of formazan at 540 nm is linearly proportional to the concentration of glutamate up to 200 μM. NBT/GDH reagent (50 μL) is added to each well by Multidrop and mixed by shaking for 30 sec on TiterMix 100, and the plates are incubated at RT for 20 min to allow color formation by the GDH reaction. Glutamate concentration is determined from formazan concentration as determined by reading OD540 nm on a SpectraMax 340.

Cell Research:

[2]

  • Cell lines: D54 cells
  • Concentrations: --
  • Incubation Time: 48 h
  • Method:

    Cell growth assays are carried out using alamarBlue. 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 礚 in each well. Fluorescence is measured at 48 hrs (AOA, BPTES) using a Victor3 plate-reader.

Animal Research:

[3]

  • Animal Models: LAP/MYC mice
  • Dosages: 12.5 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 524.68
Formula

C24H24N6O2S3

CAS No. 314045-39-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)CC(=O)NC2=NN=C(S2)CCSCCC3=NN=C(S3)NC(=O)CC4=CC=CC=C4

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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