1598424-76-0

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].

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 culturesrespectively) with good selectivity over >40 other targetsincluding LAT-2 or ASCT-2 (IC50 >10 μM).

α adrenergic receptor: ≥10 μM (IC₅₀); ASCT1: 1 nM (IC₅₀)

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[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