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Telaglenastat hydrochloride

(Synonyms: CB-839 hydrochloride)
117 Cited Publications
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Based on 117 publication(s) in Google Scholar

Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride 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 hydrochloride inudces autophagy and has antitumor activity.

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  • Reinheit : 98.03%
  • CAS. Nr.: 1874231-60-3
  • Formel: C26H25ClF3N7O3S
  • Molecular Weight:608.04
  • Speicherung:

    4°C, sealed storage, away from moisture

    * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

  • Telaglenastat hydrochloride Chemical Structure
    Telaglenastat hydrochloride Chemical Structure
  • Experimental Validation Results for Telaglenastat hydrochloride
  • Experimental Validation Results for Telaglenastat hydrochloride
  • Experimental Validation Results for Telaglenastat hydrochloride
  • Experimental Validation Results for Telaglenastat hydrochloride
  • Experimental Validation Results for Telaglenastat hydrochloride
  • Experimental Validation Results for Telaglenastat hydrochloride
  • Experimental Validation Results for Telaglenastat hydrochloride
CAS. Nr.: 1874231-60-3
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  • Telaglenastat hydrochloride Chemical Structure
    Telaglenastat hydrochloride Chemical Structure
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  • 1/16

    Telaglenastat hydrochloride purchased from MedChemExpress. Usage Cited in: Gastroenterology. 2024 May;166(5):772-786.e14. [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 hydrochloride purchased from MedChemExpress. Usage Cited in: Gastroenterology. 2024 May;166(5):772-786.e14. [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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride