IACS-010759, Mitochondrial Complex I Inhibitor (TBI4475)

Description

Product Details

Formal Name: 5-[5-Methyl-1-[[3-(4-methylsulfonylpiperidin-1-yl)phenyl]methyl]-1,2,4-triazol-3-yl]-3-[4-(trifluoromethoxyphenyl]-1,2,4-oxadiazole

Molecular Formula: C₂₅H₂₅F₃N₆O₄S

Formula Weight: 562.6

CAS Number: 1570496-34-2

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

Mitochondrial Complex I Inhibitor

Functions

Potent (IC₅₀ = 1.1 nM isolated mouse complex I) and selective inhibitor of complex I of the mitochondrial electron transport chain (OXPHOS). IACS-010759 displayed in vivo efficacy in glycolysis-deficient glioblastoma and AML models without cytotoxicity to normal cells. The lack of cytotoxicity to normal cells, as opposed to other complex I inhibitors, is attributed to its unique binding location on complex I. Complex I inhibition by IACS-010759 causes an ROS-induced decrease in the endogenous PP2A inhibitor CIP2A leading to cell death. It has also displayed potential in various chemotherapy-resistant cancer cell lines.

Application Procedures

First dissolved in DMSO (25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4475_IACS-010759_datasheet

MSDS:

TBI4475_IACS-010759_MSDS_2024

Research use only.