POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) proagent of HEX, is a potent, ENO2 -specific inhibitor of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis inhibitor.
In Vitro
POMHEX (78 nM, 8h) minimally impacts ENO1-WT glioma cells but profoundly affected ENO1-deleted cells. ?\nPOMHEX (0-720 nM) selectively induces energy stress, inhibits proliferation and triggers apoptosis in ENO1-deleted glioma cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: ENO1-deleted (D423, red), ENO1-isogenically rescued (D423 ENO1, blue) and ENO1-WT (LN319, grey) cells. Concentration: 78 nM. Incubation Time: 8 h. Result: Down-regulated cell density.
In Vivo
POMHEX (i.v., ip) injections are consistently tolerated without haemolytic anaemia at doses of up to 10 mg per kg (body weight) per day. POMHEX (i.v., 35 mg/kg) results in lethargy that prompted veterinarians to perform euthanasia . ?\nPOMHEX is rapidly hydrolysed to HemiPOMHEX in mouse plasma ex vivo, with a half-life of approximately 30 s, the half-life in human blood ex vivo was about 9min . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
