This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
GLS1 Inhibitor-4
Catalog No. T72679 CAS
2768599-97-7
GLS1 Inhibitor-4 (compound 41e) is a powerful GLS1 inhibitor, demonstrating an IC50 of 11.86 nM. It exhibits antiproliferative effects, substantial metabolic stability, and strong GLS1 binding affinity. Furthermore, it interrupts glutamine metabolism, induces ROS production, and triggers apoptosis, culminating in notable antitumor activity [1].
All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
Contact us for more batch information
Biological Description
Chemical Properties
Storage
& Solubility Information
Description
GLS1 Inhibitor-4 (compound 41e) is a powerful GLS1 inhibitor, demonstrating an IC50 of 11.86 nM. It exhibits antiproliferative effects, substantial metabolic stability, and strong GLS1 binding affinity. Furthermore, it interrupts glutamine metabolism, induces ROS production, and triggers apoptosis, culminating in notable antitumor activity [1].
In vitro
GLS1 Inhibitor-4 (compound 41e) demonstrates antiproliferative effects with IC50 values of 0.051 µM for HCT116, 0.37 µM for MDA-MB-436, 0.32 µM for CT26, and 1.34 µM for H22 cells, indicating potent activity across these cell lines [1]. It exhibits high stability in human plasma (96%) and liver microsomes, suggesting favorable pharmacokinetic properties [1]. Additionally, GLS1 Inhibitor-4 binds strongly to the GLS1 protein, with a dissociation constant (Kd) of 52 nM, reflecting high affinity [1]. It inhibits colony formation in HCT116 cells in a dose-dependent manner at concentrations of 0.1, 0.5, and 1 µM and decreases key metabolite levels downstream of glutamate at 100 and 300 nM within 12 hours [1]. This compound also dose-dependently elevates ROS levels at 30, 50, and 200 nM after 6 hours, and induces apoptosis over 24 hours [1]. Lastly, at 1 mmol/L, GLS1 Inhibitor-4 significantly reduces ATP production and suppresses aerobic glycolysis by lowering basal and maximal OCRs in HCT116 cancer cells after 12 hours [1].
In vivo
GLS1 Inhibitor-4, administered intraperitoneally at doses of 50 and 100 mg/kg twice daily for 21 consecutive days, demonstrates dose-dependent antitumor efficacy [1].
Molecular Weight
668.72
Formula
C29H27F3N10O2S2
CAS No.
2768599-97-7
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
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:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculator
Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
bottom
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.