Aclimostat

Aclimostat (ZGN-1061) (6 nM; 2-24 h) induces nearly identical gene expression changes to Beloranib (HY-14811) in HepG2 cells after 2-hour and 24-hour exposures to 6 nM, with high concordance across genes linked to metabolic efficacy^[2].
Aclimostat (1-72 h) inhibits HUVEC proliferation with an EC₅₀ of 0.24 nM after continuous 72-hour exposure, but does not affect proliferation with short-term exposures of 4 hours or less at concentrations up to 50× the EC₅₀^[2].
Aclimostat (10 nM; 2 h, assessed over 72 h post-washout) shows transient target engagement in HUVECs, with covalent binding to the MetAP2 active site declining over 72 hours after a 2-hour 10 nM exposure, and no sustained accumulation of the MetAP2 substrate THX 1-6^[2].
Aclimostat (10 nM; 2 h, assessed over 72 h post-washout) shows transient target engagement in HepG2 cells, with covalent binding to the MetAP2 active site declining over 72 hours after a 2-hour 10 nM exposure^[2].
ZGN-1061 binds strongly to human MetAP2 with a docking score of -7.2 kcal/mol, interacting with key active site residues critical for MetAP2 function^[5].
Aclimostat (1-20 nM; 4-72 h) increases p21 and reduces TM protein levels in HUVECs, but does not affect these proteins with shorter 4-hour or 8-hour exposures, and does not alter p53, vWF, or PAI-1 levels at any tested concentration or time^[2].
ZGN-1061 (0-5000 nM; 1-6 days) inhibits proliferation of A2780 and SKOV3 ovarian cancer cells, with enhanced efficacy and lower IC₅₀ values in METAP2-overexpressing SKOV3 cells compared to control SKOV3 cells, and attenuated efficacy in METAP2-knockdown A2780 cells compared to control A2780 cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.