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RU-265

Development stage: Preclinical
Lead developer: University of Colorado
Modality: Small Molecules
Administration: Intraperitoneal

Overview

RU-265 is a research-stage, inorganic small-molecule compound that acts as a potent and selective inhibitor of the mitochondrial calcium uniporter (MCU). Chemically, it is a nitrido-bridged diruthenium complex with the formula [ClRu(NH3)4(μ-N)Ru(NH3)4Cl]Cl3. Unlike its predecessor Ru360, RU-265 exhibits significantly enhanced cellular uptake, allowing it to inhibit mitochondrial calcium uptake in intact cells at low nanomolar concentrations. It has been primarily studied in academic research settings for its potential therapeutic applications in models of ischemic stroke, hypoxic/ischemic brain injury, and cardiac ischemia-reperfusion injury. Recent research presented at ASH 2023 also suggests that RU-265 can eradicate venetoclax-resistant acute myeloid leukemia (AML) stem cells by suppressing oxidative phosphorylation (OXPHOS) through the reduction of mitochondrial calcium levels.

Other names: [ClRu(NH3)4(μ-N)Ru(NH3)4Cl]Cl3

Targets

CACNA1A (P-type Calcium Channel)MCU (Mitochondrial calcium uniporter)KCNQ (Potassium voltage-gated channel subfamily Q (Kv7))

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