1. Metabolic Enzyme/Protease
    Apoptosis
  2. Enolase
    Apoptosis
  3. POMHEX

POMHEX 

Cat. No.: HY-131904
Handling Instructions

POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug 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.

For research use only. We do not sell to patients.

POMHEX Chemical Structure

POMHEX Chemical Structure

CAS No. : 2004714-34-3

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Description

POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug 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[1].

In Vitro

POMHEX (78 nM, 8h) minimally impacts ENO1-WT glioma cells but profoundly affected ENO1-deleted cells[1].
POMHEX (0-720 nM) selectively induces energy stress, inhibits proliferation and triggers apoptosis in ENO1-deleted glioma cells[1].

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

Cell Proliferation Assay[1]

Cell 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[1].
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[1].

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

Molecular Weight

423.40

Formula

C₁₇H₃₀NO₉P

CAS No.

2004714-34-3

SMILES

O=P(OCOC(C(C)(C)C)=O)(OCOC(C(C)(C)C)=O)C1C(N(O)CCC1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

POMHEXEnolaseApoptosisPhosphopyruvate hydrataseGlycolysisENO1caspaseHemiPOMHEXenergystressInhibitorinhibitorinhibit

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