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Hexokinase

Hexokinase inhibitors block the enzymes that phosphorylate glucose in the first step of glycolysis. Mammals express four hexokinase isozymes, and hexokinases I to III are inhibited by their product, glucose-6-phosphate. Hexokinase IV is covered separately in the sibling Glucokinase category. Hexokinase 2 (HK2) binds the outer mitochondrial membrane and is highly expressed in many tumors. A 2013 mouse study found HK2 to be required for tumor initiation and maintenance in lung and breast cancer models. 2-Deoxy-D-glucose is a glucose analog that is phosphorylated but not metabolized further. 3-Bromopyruvic acid and HK-2-IN-1 are listed as HK2 inhibitors, and C-02 is a proteolysis-targeting chimera that degrades HK2.

1 Item

  • C-02 (PROTAC HK2 Degrader-1)
    Cat. No.
    A23935
    CAS No.
    3033812-84-6

    C-02 (PROTAC HK2 Degrader-1)

    C-02 is a PROTAC molecule composed of the hexokinase inhibitor lonidamine linked to the cereblon ligand thalidomide. It selectively degrades hexokinase 2 in 786-O and PANC-1 cells at 20 µM. C-02 exhibits cytotoxicity across multiple cancer cell lines, with IC₅₀ values of 34.07 µM (786-O), 5.08 µM (4T1), 31.53 µM (PANC-1), 6.11 µM (HGC-27), and 21.65 µM (MCF-7), supporting its use in cancer metabolism research.

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    1 mg
    $41.00
    5 mg
    $124.00
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