V-9302
Glutamine transport inhibitor / Selective inhibitor of the alanine-serine-cysteine transporter 2 (ASCT2 or SLC1A5; IC50 = 9.0 µM rat and 9.6 µM human).1,2 It inhibited the uptake of both glutamine and possibly other amino acids in human cancer cells and reduced in vitro viability by at least 20% in more than half of 29 cancer cell lines screened.2 V-9302 decreased mTOR activity, elevated autophagy, and increased oxidative stress in multiple animal cancer models.2-5
Biochemicals & reagents
1855871-76-9
1) Schulte et al. (2016), 2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: a novel Scaffold for inhibition of ASCT2-mediated glutamine transport; Bioorg. Med. Chem. Lett., 26 1044 2) Schulte et al. (2018), Pharmacological blockade of ASCT2-dependent glutamine transport leads to antitumor efficacy in preclinical models; Nat. Med., 24 194 3) Zhang (2020), ASCT2 (SLC1A5)-dependent glutamine uptake is involved in the progression of head and neck squamous cell carcinoma; Br. J. Cancer, 122 82 4) Jin et al. (2020), A powerful drug combination strategy targeting glutamine addiction for the treatment of human liver cancer; Elife, 9 e56749 5) Edwards et al. (2021), Selective glutamine metabolism inhibition in tumor cells improves antitumor T lymphocyte activity in triple-negative breast cancer J. Clin. Invest., 131 e140100
-20°C
PATHWAY: Amino acid metabolism; Mitochondrial function; mTOR -- RESEARCH AREA: Oxidative stress; Cell death; Stem cells -- DISEASE AREA: Cancer; Osteoporosis