BPTES

For research use only.

Catalog No.S7753

25 publications

BPTES Chemical Structure

CAS No. 314045-39-1

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.

Selleck's BPTES has been cited by 25 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 MY\DfZRwfG:6aXPpeJkh[XO|YYm= MmXxOkBl[Xm| MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IH3lZZN2emWmIH;uJFZ1cCCmYYmgZpkhcGWvb3P5eI9u\XS{eTygTWM2OD1{Lk[xJO69VQ>? M2P4TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUi4PFA{Lz5{Nkm4PFgxOzxxYU6=
MDA-MB-231 MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn3PO|IhcHK| NHu2bGFIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGlEPTBiPTC2Mlgh|ryPLh?= NV7DOXkzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2NFkyODFpPkK4OlA6OTBzPD;hQi=>
Aspc-1 M{fWTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NInIeYU4OiCqcoO= NULtVYxkT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hSXOyYz2xJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSBzMD6yJO69VS5? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZyOUGwNUc,Ojh4MEmxNFE9N2F-
HCC827 NHS3d4VEgXSxdH;4bYNqfHliYYPzZZk> MYq0PEBpenN? MlvKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6g[ZJtd3SrbnniMZJme2m|dHHueEBJS0N6MkegZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IFPDT|gh[XO|YYmsJGlEPTBiPTC0Nk41KM7:TT6= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF5NEGwOUc,OjhzN{SxNFU9N2F-
HT1080 MXrDfZRwfG:6aXPpeJkh[XO|YYm= NGfYU2g1QCCqcoO= NHHGTnFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXDFyOECgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiNEigbJJ{KGK7IFPDT|gh[XO|YYmsJGlEPTBiPTC0O{44OiEQvF2u NYfzNoF[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixO|QyODVpPkK4NVc1OTB3PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
γH2AX; 

PubMed: 29107960     


MEF, PC3, or HT1080 cells were treated with 50 μM DON or 50 μM BPTES for 48 hours.

c-Myc / KLF4 / SOX2 / OCT4 / NANOG / GLS1; 

PubMed: 30555042     


HCCLM3 cells were treated with 5, 10, or 20 μM 968 or BPTES for 48 h, then Western blot was employed to detect the expression of stemness markers. 

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

Kinase Assay:

[1]

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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]

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  • 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.


    (Only for Reference)
Animal Research:

[3]

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  • Animal Models: LAP/MYC mice
  • Dosages: 12.5 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (190.59 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 524.68
Formula

C24H24N6O2S3

CAS No. 314045-39-1
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC=C(C=C1)CC(=O)NC2=NN=C(S2)CCSCCC3=NN=C(S3)NC(=O)CC4=CC=CC=C4

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID