Uses
BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research[1][2].
Biological Activity
Potent and selective alanine serine cysteine transporter-1 (ASC-1; SLC7A10) inhibitor th at effectively blocks ASC-1-mediated cellular D-Ser uptake.
BMS-466442 is a selective alanine serine cysteine transporter-1 (ASC-1) inhibitor (D-Ser uptake IC50 = 36.8 nM and 19.7 nM using HEK human ASC-1 transfectants or primary r at embryonic cortical cultures, respectively) with good selectivity over >40 other targets, including LAT-2 or ASCT-2 (IC50 >10 μM).
IC 50
α adrenergic receptor: ≥10 μM (IC
50); ASCT1: 1 nM (IC
50)
References
[1] Brown JM, et al. In vitro Characterization of a small molecule inhibitor of the alanine serine cysteine transporter -1 (SLC7A10). J Neurochem. 2014 Apr;129(2):275-83. DOI:
10.1111/jnc.12618[2] Torrecillas IR, et al. Inhibition of the Alanine-Serine-Cysteine-1 Transporter by BMS-466442. ACS Chem Neurosci. 2019 May 15;10(5):2510-2517. DOI:
10.1021/acschemneuro.9b00019
