U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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A sulfide ion is composed of a lone sulfur atom. Its charge is negative two, giving sulfides this formula: S^2-. Sulfide is a strong base, so solutions of sulfide in water are basic, due to hydrolysis. One well-known ionic compound with a sulfide ion is H_2S. The infamous rotten-egg smell often associated with sulfur originates from this compound. Sodium sulfide nonahydrate is used in the formation of surface functionalized cadmium sulfide quantum dots.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oxime (CITCO) is a novel potent and selective agonist for the human orphan nuclear receptor CAR (constitutive androstane receptor). CITCO displayed an EC50 of 49 nM in a CAR FRET assay and showed 50-fold selectivity for CAR over PXR. CITCO displayed no activity against a panel of 15 other nuclear receptors at a concentration of 10 µM. In hepatocytes CITCO induced CAR nuclear translocation and induced the CAR target gene CYP2B6. The cell proliferation of several ovarian cell lines expressing CAR significantly increased when CITCO was combined with anticancer agents compared with any anticancer agent alone. The up-regulation of MDR1 and UGT1A1 by anticancer agents was further enhanced in the presence of CITCO. Combination of CITCO with any anticancer agents significantly enhanced CAR-mediated transcription compared with any anticancer agents alone and CAR down-regulation completely inhibited the transcription in the presence of CITCO and/or anticancer agents. Inhibition of CAR pathway could be a novel therapeutic approach for the augmentation of sensitivity to anticancer agents, or to overcome resistance, in the treatment of ovarian cancer. CITCO has being shown to inhibit growth and expansion of brain tumour stem cells. CITCO induced a dose-dependent decrease in growth and expansion of CD133(+) BTSCs as gliospheres in culture. Cell cycle arrest and apoptosis in BTSCs were induced by CITCO, but not in normal astrocytes. Growth of s.c BTSC xenograft in nude mice was also inhibited by CITCO. CITCO inhibits the growth and expansion of BTSCs, suggesting the use of CAR agonists for the treatment of brain tumour.
T0901317 is a potent, high affinity liver X receptors (LXRs) agonist. It upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and high-density lipoproteins metabolism. It also exhibits inverse agonist activity at constitutive androstane receptors (CARs). T0901317 activates bile acid farnesoid X receptors (FXRs), and it is 10-fold more potent than natural FXR ligand chenodeoxycholic acid.
Androstanol is a steroid acting as the inverse agonist of constitutive androstane receptor. In addition, androstanol activates pregnane X receptor. In animal models, it protects from drug-induced liver injury. Androstanol appears to be a pheromone.
Datiscetin is a yellow plant dye from the flavonol group. It exhibited inhibitory activity against methicillin-resistant Staphylococcus aureus (MRSA). Datiscetin demonstrated antioxidant activity – it inhibits CCl4-induced microsomal lipid peroxidation and behaved as potent scavenger of the superoxide anion radicals. Datiscetin activated the human constitutive androstane receptor. It inhibited amyloid beta-42 protein aggregation. Datiscetin interacts with amyloid beta-42 protein directly, with monomers and small aggregates.
A sulfide ion is composed of a lone sulfur atom. Its charge is negative two, giving sulfides this formula: S^2-. Sulfide is a strong base, so solutions of sulfide in water are basic, due to hydrolysis. One well-known ionic compound with a sulfide ion is H_2S. The infamous rotten-egg smell often associated with sulfur originates from this compound. Sodium sulfide nonahydrate is used in the formation of surface functionalized cadmium sulfide quantum dots.
A sulfide ion is composed of a lone sulfur atom. Its charge is negative two, giving sulfides this formula: S^2-. Sulfide is a strong base, so solutions of sulfide in water are basic, due to hydrolysis. One well-known ionic compound with a sulfide ion is H_2S. The infamous rotten-egg smell often associated with sulfur originates from this compound. Sodium sulfide nonahydrate is used in the formation of surface functionalized cadmium sulfide quantum dots.
A sulfide ion is composed of a lone sulfur atom. Its charge is negative two, giving sulfides this formula: S^2-. Sulfide is a strong base, so solutions of sulfide in water are basic, due to hydrolysis. One well-known ionic compound with a sulfide ion is H_2S. The infamous rotten-egg smell often associated with sulfur originates from this compound. Sodium sulfide nonahydrate is used in the formation of surface functionalized cadmium sulfide quantum dots.
A sulfide ion is composed of a lone sulfur atom. Its charge is negative two, giving sulfides this formula: S^2-. Sulfide is a strong base, so solutions of sulfide in water are basic, due to hydrolysis. One well-known ionic compound with a sulfide ion is H_2S. The infamous rotten-egg smell often associated with sulfur originates from this compound. Sodium sulfide nonahydrate is used in the formation of surface functionalized cadmium sulfide quantum dots.