KP1339 (KP1019 sodium) is a ruthenium-indazole complex-based anticancer agent that induces pronounced apoptosis in sensetive cancer cells (Capan1/HCT116/SW480/KB-3-1 IC50 by MTT assay = 44/50/145/170 µM) via ER homeostasis disruption and caspase 8 activation due to depletion of key cellular chaperones, including BiP/GRP78/HSPA5, in combination with enhanced protein damage. When administered in vivo, KP1339 exhibits anti-tumor efficacy in the murine SA-1 fibrosarcoma model (10.5, 21.0, 42.0 mg/150 µL/kg i.v.).
Ruthenium-indazole complex-based anticancer agent in cultures and in vivo via ER homeostasis disruption by depleting chaperones, including BiP/GRP78/HSPA5.
Interaction with Ribosomal Proteins Accompanies Stress Induction of the Anticancer Metallodrug BOLD-100/KP1339 in the Endoplasmic Reticulum
Angewandte Chemie (International ed. in English), 60, 5063-5068 (2021)
Sensitivity towards the GRP78 inhibitor KP1339/IT-139 is characterized by apoptosis induction via caspase 8 upon disruption of ER homeostasis
Cancer Letters, 404, 79-88 (2017)
The influence of electroporation on cytotoxicity of anticancer ruthenium(III) complex KP1339 in vitro and in vivo
Anticancer Research, 30, 2055-2063 (2010)
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