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POMHEX 

Cat. No. M29100
POMHEX  Structure
Size Price Availability Quantity
5mg USD 430  USD430 In stock
10mg USD 750  USD750 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 423.4
Formula C17H30NO9P
CAS Number 2004714-34-3
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Victoria C Yan, et al. J Med Chem. Prodrugs of a 1-Hydroxy-2-oxopiperidin-3-yl Phosphonate Enolase Inhibitor for the Treatment of ENO1-Deleted Cancers

[2] Sunada Khadka, et al. Cancer Metab. Impaired anaplerosis is a major contributor to glycolysis inhibitor toxicity in glioma

[3] Yu-Hsi Lin, et al. Nat Metab. An enolase inhibitor for the targeted treatment of ENO1-deleted cancers

[4] Victoria C Yan, et al. ACS Pharmacol Transl Sci. Comparative Pharmacology of a Bis-Pivaloyloxymethyl Phosphonate Prodrug Inhibitor of Enolase after Oral and Parenteral Administration

Related Enolase Products
SF2312 

SF2312, a natural phosphonate antibiotic (Antibiotic), is a highly potent Enolase inhibitor with IC50s of 37.9 nM and 42.5 nM for human recombinant ENO1 and ENO2, respectively. SF2312 is active against bacteria under anaerobic conditions.

  Catalog
Abmole Inhibitor Catalog




Keywords: POMHEX  supplier, Enolase, inhibitors, activators


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