An inhibitor of Atox1 and CCS; binds to purified Atox1 and CCS (Kds = 6.8 and 8.2 μM

DC_AC50 – 5 mg

Brand:
Cayman
CAS:
497061-48-0
Storage:
-20
UN-No:
Non-Hazardous - /

DC_AC50 is an inhibitor of the copper-trafficking proteins Atox1 and CCS.{53558} It binds to purified Atox1 and CCS (Kds = 6.8 and 8.2 μM, respectively) and inhibits the interaction between Atox1 and domain 4 of the Cu+-ATPase ATP7B in the presence of zinc in a FRET-based assay when used at a concentration of 100 μM. DC_AC50 increases copper and reactive oxygen species (ROS) levels and decreases COX activity and lipid biosynthesis in H1299 cells when used at a concentration of 10 μM. It inhibits the proliferation of H1299, K562, MDA-MB-231, and 212LN cancer cells, but not PIG1, HDF, HaCaT, or MCF-10A cells, in a concentration-dependent manner. DC_AC50 (100 mg/kg per day) reduces tumor growth in an H1299 mouse xenograft model.  

 

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Description

An inhibitor of Atox1 and CCS; binds to purified Atox1 and CCS (Kds = 6.8 and 8.2 μM, respectively); inhibits the interaction between Atox1 and domain 4 of ATP7B in the presence of zinc in a FRET-based assay at 100 μM; increases copper and ROS levels and decreases COX activity and lipid biosynthesis in H1299 cells at 10 μM; inhibits the proliferation of H1299, K562, MDA-MB-231, and 212LN cancer cells, but not PIG1, HDF, HaCaT, or MCF-10A cells, in a concentration-dependent manner; reduces tumor growth in an H1299 mouse xenograft model at 100 mg/kg per day

Formal name: 3-amino-N-(2-bromo-4,6-difluorophenyl)-6,7-dihydro-5H-cyclopenta[b]thieno[3,2-e]pyridine-2-carboxamide

Synonyms: 

Molecular weight: 424.3

CAS: 497061-48-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ox Stress Reagents||Research Area|Cancer||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway||Research Area|Oxidative Stress & Reactive Species|Pro-oxidant Activity||Research Area|Oxidative Stress & Reactive Species|Reactive Oxygen

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