C-02 |
| Catalog No.GC91442 |
C-02 es una quimera dirigida a la proteólisis (PROTAC) compuesta por el inhibidor de hexoquinasa lonidamina unido al ligando cereblón talidomida.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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