Name: BPTES
Brand: Selleck Chemicals
SKU: S7753
Availability: InStock
Rating: 5 (60 reviews)

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Quality Control

Batch: Purity: >97%

Cited in Nature Medicine for its top-tier quality
COA
Datasheet
SDS

Cited in Nature Medicine for its top-tier quality
COA
Datasheet
SDS

Cited in Nature Medicine for its top-tier quality
COA
NMR
Datasheet
SDS

Cited in Nature Medicine for its top-tier quality
COA
NMR
Datasheet
SDS

Cited in Nature Medicine for its top-tier quality
COA
NMR
Datasheet
SDS

97

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease
Other Glutaminase Inhibitors	Telaglenastat (CB-839) JHU-083 GK921 LDN-27219 JHU395 6-Diazo-5-oxo-L-norleucine (Diazooxonorleucine) UPGL00004 IACS-6274 Glutaminase C-IN-1 Sirpiglenastat (DRP-104)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
MDA-MB-231 cell	Cytotoxicity assay	6 days	Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry, IC50=2.61 μM	26988803
MDA-MB-231	Growth inhibition assay	72 hrs	Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTS assay, IC50 = 6.8 μM.	28609101
Aspc-1	Growth inhibition assay	72 hrs	Growth inhibition of human Aspc-1 cells after 72 hrs by MTS assay, IC50 = 10.2 μM.	28609101
HCC827	Cytotoxicity assay	48 hrs	Cytotoxicity against human erlotinib-resistant HCC827 cells assessed as growth inhibition after 48 hrs by CCK8 assay, IC50 = 42.4 μM.	28174105
HT1080	Cytotoxicity assay	48 hrs	Cytotoxicity against human HT1080 cells assessed as growth inhibition after 48 hrs by CCK8 assay, IC50 = 47.72 μM.	28174105
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (95.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (2.38mM)	Taking the 1 mL working solution as an example, add 50 μL 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.400mg/ml (0.76mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.400mg/ml (0.76mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	524.68	Formula	C₂₄H₂₄N₆O₂S₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	314045-39-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin 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

Mechanism of Action

Targets/IC₅₀/Ki	Glutaminase GLS1 (KGA) 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. This compound preferentially slows cell growth in D54 cells with mutant IDH1. It also inhibits glutaminase activity, lowers glutamate and α-KG levels, and increases glycolytic intermediates. This chemical (10 μM) inhibits cell growth of mHCC 3–4 cells derived from LAP/MYC tumors. It also inhibits growth of a MYC-dependent P493 cells by blocking DNA replication, leading to cell death and fragmentation.
Kinase Assay	Glutaminase Inhibition: Cell Free Assay
Kinase 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.
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. This compound (200 μg/mouse, i.p.) also inhibits tumor cell growth in mice harboring P493 tumor xenografts.
References	[1] http://www.google.com/patents/US6451828 [2] https://pubmed.ncbi.nlm.nih.gov/21045145/ [3] https://pubmed.ncbi.nlm.nih.gov/25915584/

Applications

Methods	Biomarkers	Images	PMID
Western blot	γH2AX c-Myc / KLF4 / SOX2 / OCT4 / NANOG / GLS1		29107960

Tech Support

Handling Instructions

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BPTES Glutaminase inhibitor

Chemical Structure

Molecular Weight: 524.68