| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg | |||
| 50mg | |||
| Other Sizes |
| Targets |
POMHEX targets ENO2 (enolase 2), a key enzyme in the glycolysis pathway. Enolase catalyzes the conversion of 2-phosphoglycerate to phosphoenolpyruvate in glycolysis. By inhibiting ENO2, POMHEX blocks glycolysis and reduces ATP production in cancer cells. The compound is particularly effective against ENO1-deficient cells, which are dependent on ENO2 for glycolysis. This selective vulnerability makes ENO1-deficient tumors a promising target for POMHEX therapy.
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| ln Vitro |
POMHEX (78 nM, 8h) significantly affects ENO1-deficient cells but has no impact on ENO1-WT glioma cells [1]. POMHEX (0-720 nM) specifically causes energy stress, suppresses growth, and initiates death in glioma cells lacking ENO1 [1].
In vitro, POMHEX displays low nanomolar activity against ENO1-deficient cells. The compound inhibits ENO2 and blocks glycolysis, leading to reduced ATP production and cell death in ENO1-deficient cancer cells. POMHEX has been shown to have potent anticancer effects in cells with deficiencies in oxidative metabolism. These in vitro studies demonstrate the compound's potential as a targeted cancer therapy. |
| ln Vivo |
Hemolytic anemia was consistently avoided with POMHEX (iv, ip) injections at doses up to 10 mg/kg (body weight) per day. POMHEX (intravenous, 35 mg/kg) makes patients drowsy, which leads vets to start the euthanasia process [1]. In isolated mouse plasma, POMHEX hydrolyzes quickly to Hemi POMHEX, which has a half-life of roughly 30 seconds, while in isolated human blood, it has a half-life of almost 9 minutes [1].
In vivo, POMHEX has shown good anticancer effects in ENO1-deficient tumor models. The compound is being studied for the treatment of gliomas and other tumors with deficiencies in oxidative metabolism. Its ability to selectively inhibit cancer cell metabolism makes it a valuable tool for developing novel cancer therapies. Further in vivo studies are ongoing to evaluate its efficacy and safety. |
| Enzyme Assay |
The in vitro enzyme inhibition assay for POMHEX measures its ability to inhibit ENO2 enzymatic activity. The assay is performed using purified ENO2 enzyme and the substrate 2-phosphoglycerate. The reaction is monitored by measuring the production of phosphoenolpyruvate or by coupled enzyme assays. IC50 values are calculated from dose-response curves. Selectivity is assessed by testing the compound against ENO1 and other glycolytic enzymes.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: ENO1-deleted (D423, red), ENO1-isogenically rescued (D423 ENO1, blue) and ENO1-WT (LN319, gray) cells. Tested Concentrations: 78 nM. Incubation Duration: 8 h. Experimental Results: Down-regulated cell density. In vitro cellular studies are conducted using ENO1-deficient and ENO1-proficient cancer cell lines. Cells are treated with POMHEX at various concentrations (typically nM to μM ranges) for defined time periods. Cell viability is assessed using MTT or CellTiter-Glo assays. Glycolysis is measured by assessing lactate production, glucose uptake, or extracellular acidification rate. ATP levels are measured using luminescence-based assays. Apoptosis is assessed by measuring caspase activity or Annexin V staining. |
| Animal Protocol |
In vivo animal experiments are performed using xenograft models of ENO1-deficient tumors. Tumor-bearing mice are administered POMHEX via various routes at different doses. Tumor volume is measured over time, and endpoints include tumor growth inhibition and survival. Pharmacodynamic studies evaluate glycolysis inhibition and ATP depletion in tumor tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of POMHEX include its cell permeability and solubility. The compound has a molecular weight of 423.40 g/mol and molecular formula C17H30NO9P. It appears as a solid and should be stored at -20°C for stability. The compound is a POM prodrug, which enhances its cell permeability. Storage conditions should be optimized to maintain stability.
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| Toxicity/Toxicokinetics |
Toxicological data for POMHEX are derived from preclinical studies. The compound is for research use only and not intended for human therapeutic applications. No significant toxicity has been reported at effective doses in animal studies. Standard safety precautions should be followed when handling the compound due to its potent biological activity. Long-term toxicity and carcinogenicity studies have not been conducted.
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| References | |
| Additional Infomation |
POMHEX is a racemic mixture and a cell-permeable POM prodrug of HEX that specifically inhibits ENO2. It is a potent glycolysis inhibitor and displays low nanomolar activity against ENO1-deficient cells. POMHEX has shown good anticancer effects in ENO1-deficient tumor models and is being studied for the treatment of gliomas and other tumors with oxidative metabolism deficiencies. The compound has the molecular formula C17H30NO9P and molecular weight of 423.40 g/mol.
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| Molecular Formula |
C17H32NO9P
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|---|---|
| Molecular Weight |
425.411046981812
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| Exact Mass |
423.165
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| CAS # |
2004714-34-3
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| Related CAS # |
Hex;2004714-32-1
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| PubChem CID |
122540908
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| Appearance |
White to light yellow solid powder
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| LogP |
1.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
28
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| Complexity |
600
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCN(O)C(C1P(=O)(OCOC(C(C)(C)C)=O)OCOC(O)C(C)(C)C)=O
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| InChi Key |
TVFIFFUSHZDTKT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H30NO9P/c1-16(2,3)14(20)24-10-26-28(23,12-8-7-9-18(22)13(12)19)27-11-25-15(21)17(4,5)6/h12,22H,7-11H2,1-6H3
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| Chemical Name |
[2,2-dimethylpropanoyloxymethoxy-(1-hydroxy-2-oxopiperidin-3-yl)phosphoryl]oxymethyl 2,2-dimethylpropanoate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (236.18 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3507 mL | 11.7534 mL | 23.5067 mL | |
| 5 mM | 0.4701 mL | 2.3507 mL | 4.7013 mL | |
| 10 mM | 0.2351 mL | 1.1753 mL | 2.3507 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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