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Telaglenastat

(別名: CB-839)
110 Cited Publications
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Based on 110 publication(s) in Google Scholar

Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity.

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  • 純度: 99.82%
  • CAS 番号: 1439399-58-2
  • 分子式: C26H24F3N7O3S
  • 分子量:571.57
  • 保管条件:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 1 year , -20°C, 6 months
  • Telaglenastat Chemical Structure
    Telaglenastat 構造式
  • Experimental Validation Results for Telaglenastat
  • Experimental Validation Results for Telaglenastat
  • Experimental Validation Results for Telaglenastat
  • Experimental Validation Results for Telaglenastat
  • Experimental Validation Results for Telaglenastat
  • Experimental Validation Results for Telaglenastat
  • Experimental Validation Results for Telaglenastat
CAS 番号: 1439399-58-2
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  • Telaglenastat Chemical Structure
    Telaglenastat Chemical Structure
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    Telaglenastat purchased from MedChemExpress. Usage Cited in: Gastroenterology. 2024 Jan 24:S0016-5085(24)00064-7. [Abstract]

    Customer Validation
     Phase-contrast images of dysplastic organoids treated with dimethyl sulfoxide (DMSO; vehicle), GSK2837808A (LDH inhibitor; 10 μmol/L), 6-aminonicotinamide (6-AN, glucose-6-phosphate dehydrogenase [G6PD] inhibitor; 50 μmol/L), telaglenastat (GLS1 inhibitor; 1 μmol/L) for 3 days.

  • 1/16

    Telaglenastat purchased from MedChemExpress. Usage Cited in: Gastroenterology. 2024 Jan 24:S0016-5085(24)00064-7. [Abstract]

    Customer Validation
     Phase-contrast images of dysplastic organoids treated with dimethyl sulfoxide (DMSO; vehicle), GSK2837808A (LDH inhibitor; 10 μM), 6-aminonicotinamide (G6PD inhibitor; 50 μM), telaglenastat (GLS1 inhibitor; 1 μM) for 3 days.

  • 1/16

    Telaglenastat purchased from MedChemExpress. Usage Cited in: Pathol Int. 2023 May;73(5):181-187. [Abstract]

    Customer Validation
     Telaglenastat (1, 2.5, 5, 10 μM; 5 days) inhibits the proliferation of DeGISTL1 cells dose-dependently.

  • 1/16

    Telaglenastat purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 Jun;40(6):814-822. [Abstract]

    Customer Validation
     The protein expression levels of the genes related to cell cycle and metabolism are detected by immunoblotting using the corresponding antibodies in H1299 cells treated with 20 nM THZ1 alone or in combination with 500 nM CB-839 for 48 h.

  • 1/16

    Telaglenastat purchased from MedChemExpress. Usage Cited in: Am J Respir Cell Mol Biol. 2018 Mar;58(3):378-390. [Abstract]

    Customer Validation
     Human normal lung fibroblasts are treated as in A. Levels of the indicated proteins are determined by Western blotting. CB-839 remarkably inhibits the expression of Collagens I and III in myofibroblasts.

  • 1/16

    Telaglenastat purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Oct 2;504(2):415-421. [Abstract]

    Customer Validation
     PC3 cells are treated with indicated doses of CB-839 for 24 h after c-Myc overexpression. Cells are then harvested for the determination of indicated proteins levels.

  • 1/16

    Telaglenastat purchased from MedChemExpress. Usage Cited in: Blood Adv. 2017 Jul 14;1(17):1296-1305. [Abstract]

    Customer Validation
     The drug could be detected through MS only in the plasma from rats receiving its administration, confirming its systemic bioavailability after the treatment. Labeling scheme in panels B and C is based on the presence (+) or absence (−) of shock, DMSO (control for vehicle to the drug CB-839), and glutaminase inhibitor. Three columns are graphed per each group, indicating baseline, postshock, and end-of-shock values.

  • Telaglenastat