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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].

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GLS1 Inhibitor-4 Chemical Structure
GLS1 Inhibitor-4, CAS 2768599-97-7
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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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

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

GLS1 Inhibitor-4 2768599-97-7 Proteases/Proteasome Glutaminase inhibitor inhibit

 

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