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POMHEX

CAS No. : 2004714-34-3

產(chǎn)品活性：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.

研究領(lǐng)域：Metabolic Enzyme/Protease  |  Apoptosis

作用靶點(diǎn)：Enolase  |  Apoptosis

In Vitro: POMHEX (78 nM, 8h) minimally impacts ENO1-WT glioma cells but profoundly affected ENO1-deleted cells.
POMHEX (0-720 nM) selectively induces energy stress, inhibits proliferation and triggers apoptosis in ENO1-deleted glioma cells.

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.
POMHEX 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.

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