A mitochondrial complex I inhibitor and inducer of ferroptosis; decreases ATP-dependent luciferase reporter activity and ATP levels in H1299luc cells; induces production of ROS

BAY 87-2243 – 5 mg

Brand:
Cayman
CAS:
1227158-85-1
Storage:
-20
UN-No:
Non-Hazardous - /

BAY 87-2243 is an inhibitor of mitochondrial complex I, also known as NADH:ubiquinone oxidoreductase, and an inducer of ferroptosis.{46511,46512} It decreases ATP-dependent luciferase reporter activity and ATP levels in H1299luc cells, effects that can be reversed by addition of the mitochondrial complex II substrate succinate or expression of the S. cerevisiae complex I ortholog Ndi1 NADH dehydrogenase.{46511} BAY 87-2243 induces production of reactive oxygen species (ROS), increases α-tocopherol-sensitive lipid peroxidation, and decreases glutathione (GSH) levels in SK-MEL-28 and G361 melanoma cells, effects that can be partially reversed by the ferroptosis inhibitor ferrostatin-1 (Item No. 17729) and overexpression of GPX4 or potentiated by GPX4 knockdown.{46512} In vivo, BAY 87-2243 (0.5-4 mg/kg) reduces tumor weight, hypoxia-inducible factor-1α (HIF-1α) levels, and HIF-1α target gene expression in an H460 mouse xenograft model.{46511} It also reduces tumor growth in the MEXF 276 and MEXF 1732 melanoma patient-derived xenograft (PDX) mouse models.{46513}  

 

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SKU: 28626 - 5 mg Category:

Description

A mitochondrial complex I inhibitor and inducer of ferroptosis; decreases ATP-dependent luciferase reporter activity and ATP levels in H1299luc cells; induces production of ROS, increases α-tocopherol-sensitive lipid peroxidation, and decreases GSH levels in SK-MEL-28 and G361 melanoma cells; reduces tumor weight, HIF-1α levels, and HIF-1α target gene expression in an H460 mouse xenograft model from 0.5-4 mg/kg; reduces tumor growth in the MEXF 276 and MEXF 1732 melanoma PDX mouse models

Formal name: 1-cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]-piperazine

Synonyms: 

Molecular weight: 525.5

CAS: 1227158-85-1

Purity: ≥98%

Formulation: A crystalline solid

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