Elesclomol (STA-4783) is a novel oxidative stress inducer that acts on tumor cells and promotes their apoptosis, and is a strong copper ion carrier that can be used for copper death research. By Affymetrix microarray analysis, Elesclomol significantly induced the expression of heat shock stress response genes and metallothionein genes in Hs294T cells treated at 100 nM for 6 h. Ramos Burkitt's lymphoma B cells were treated with Elesclomol (100 nM) for 1 h and 6 h, respectively, and the Hsp70 RNA level was rapidly increased by 4.8 times and 160 times, which was consistent with the intracellular ROS content. After 0.5 h and 6 h Elesclomol treatment, ROS content increased by 20% and 385%, respectively. Antioxidant N-acetylcysteine (NAC) and Tiron pretreatment could inhibit the induction of Hsp70. HSB2 cells treated with 200 nM Elesclomol for 18 h could induce oxidative stress and increase the apoptotic cells in early stage and late stage by 3.7 times and 11 times, respectively. The above effects could be completely inhibited by NAC, but had no effect on normal cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 40 mg/mL|
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8-hydroxyquinoline is a mono-proton bicyclic chelator that is used as a preservative, disinfectant, and insecticide and as a transcription inhibitor. Is a kind of antiseptic with mild inhibition of fungi, bacteria, insect repellent, killing amoeba characteristics, is a strong copper ion carrier, can be used for copper death research.
Disulfiram is used in the study of chronic alcoholism with acute sensitivity to alcohol and is a potent copper ion-carrier that can be used in the study of copper death.
Zinc Pyrithione is an anti-fungal and anti-bacterial drug that disrupts membrane transport by blocking proton pumps and is a potent copper ion carrier that can be used in copper death studies.
NSC 319726 is a p53(R175) mutant activator that inhibits the growth of cells expressing mutant p53. It acts on p53(R175) mutant with IC50 of 8 nM and has no inhibition on p53 wild-type cells. It is a powerful copper ion-carrier and can be used for the study of copper death.
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