C-02 |
Catalog No.GC91442 |
C-02 est une chimère de ciblage de protéolyse (PROTAC) composée de l'inhibiteur d'hexokinase lonidamine lié au ligand cereblon thalidomide.
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Sample solution is provided at 25 µL, 10mM.
C-02 is a proteolysis-targeting chimera (PROTAC) composed of the hexokinase inhibitor lonidamine linked to the cereblon ligand thalidomide .1 It induces degradation of hexokinase 2 in 786-O and PANC-1 cells when used at a concentration of 20 µM. C-02 is cytotoxic to 786-O, 4T1, PANC-1, HGC-27, and MCF-7 cancer cells (IC50s = 34.07, 5.08, 31.53, 6.11, and 21.65 µM, respectively). It reduces the extracellular acidification rate (ECAR) and oxygen consumption rate (OCR) in 4T1 cells, indicating inhibition of glycolysis and mitochondrial damage, respectively, when used at a concentration of 20 µM. In vivo, C-02 (50 mg/kg) reduces tumor volume and induces intratumoral cytokine accumulation and pyroptosis in a 4T1 murine mammary carcinoma model.
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