ML241 is a novel and potent p97 inhibitor which inhibits p97 ATPase with an IC50 value of 100 nM. ML241 inhibited degradation of a p97-dependent but not a p97-independent proteasome substrate in a dual-reporter cell line. ML241 also impaired the endoplasmic-reticulum-associated degradation (ERAD) pathway. The AAA ATPase p97 is a critical factor in maintaining protein […]
Etofibrate, the ethandiol-1,2 diester of the nicotinic and clofibric acid, is a combination of conjugated clofibrate and niacin that is used to treat hyperlipemia. Etofibrate treatment heightens the cytosolic glycerol-3-phosphate dehydrogenase activity and the total carnitine concentration in the liver of rats, whereas it reduces triacylglycerol and cholesterol concentrations. Etofibrate decreases plasma levels of cholesterol, […]
Acipimox (also known as Olbemox; K-9321; Olbetam) is a novel and potent niacin derivative used as a hypolipidemic agent. It is used in low doses and may have less marked adverse effects, although it is unclear whether the recommended dose is as effective as are standard doses of nicotinic acid. Acipimox inhibits the production of […]
BRD7552 is an inducer of transcription factor PDX1, which increases insulin expression. In human cells, BRD7552 upregulated the expression of PDX1 via epigenetically altering PDX1 promoter area [3]. BRD7552 was discovered as a PDX1 inducer in a cell-based phenotypic screening assay. It was used to induce the expression of PDX1. In PANC-1 cells, BRD7552 up-regulated […]
Nicaraven is a hydroxyl radical scavenger with antivasospastic and neuroprotective effects. Nicaraven causes a dose-dependent, slight inhibition of poly (ADP-ribose) synthetase activation, possibly due to a direct inhibitory effect on the catalytic activity of poly (ADP-ribose) synthetase in RAW murine macrophages stimulated with peroxynitrite. Nicaraven partially protects against the peroxynitrite-induced suppression of mitochondrial respiration in […]
Dimesna (also called BNP-7787) is an uroprotective agent used to decrease urotoxicity caused by anticancer drugs such cisplatin. It reacts with acrolein and other urotoxic metabolites of oxazaphosphorine class of antitumor drugs such as cyclophosphamide or ifosfamide to form stable, non-urotoxic compounds.Dimesna modulates paclitaxel-induced hyperpolymerization of MTP in a dose-dependent manner, and mesna, an in […]
Discontinued (DEA controlled substance). Etizolam is a benzodiazepine analog and a specific platelet-activating factor (PAF) antagonist with anti-anxiety activity. Etizolam is marketed under the brand name Etilaam, Etizola, Sedekopan, Etizest, Pasaden or Depas. The etizolam molecule differs from a benzodiazepine in that the benzene ring has been replaced by a thiophene ring and triazole ring […]
Azeliragon 2HCl (formerly TTP-488 dihydrochloride; PF04494700) is an orally bioactive RAGE (Receptor for Advanced Glycation End products) inhibitor that has the potential for the treatment of mild-to-moderate AD/Alzheimer’s disease and cerebral amyloid angiopathy. RAGE is a pattern recognition receptor that affects the movement of amyloid (a biomarker for Alzheimer’s disease) into the brain. In preclinical […]
FPH2 (also known as BRD-9424) is able to promote differentiation of iPS-derived hepatocytes. In vitro, FPH2 induced functional proliferation of hepatocytes and might be useful for expanding mature human primary hepatocytes. In human primary hepatocytes, FPH2 increased the number of nuclei undergoing mitosis and hepatocyte nuclei count in a concentration dependent way. Also, FPH2 (40 […]
Pramiracetam (also known as CI-879) is investigated for its cognition-enhancing properties. A lower dosage of pramiracetam (100 mg/kg i.p.) was inadequate on NOS mRNA expression and chemical action. Interestingly, organization of pramiracetam (300 mg/kg i.p.) in rats pretreated (24 h before) with lithium chloride (LiCl) (3 mEq/kg i.p.) yielded a 40% expansion in cortical NOS […]