| Name | NB-598 |
| Description | NB-598 is an effective and competitive inhibitor of squalene epoxidase. It suppresses triglyceride biosynthesis through the farnesol pathway. |
| Kinase Assay | Caco-2 cells are grown in a 58 cm2 plastic dish with medium A for 13 days. The cells are washed with medium B, and then cultured with medium B including cholesterol-micelle and each compound. The compound is dissolved in Me2SO, and the final concentration of Me2SO is 0.1%(v/v). After 18 hr of incubation, the cells are washed extensively with phosphate-buffered saline (PBS) to remove the compound. Microsomes are prepared as described above. The reaction mixture (0.2 mL) consisted of 0.1 mg microsomes, 0.25% BSA and 40 PM [14C]oleoyl CoA in buffer A. To avoid the effects of endogenous cholesterol, liposome (2 mol of cholesterol: 1 mol of phosphatidylcholine) [15] is added to the reaction mixture. The microsomes are preincubated for 1 hr with or without exogenous cholesterol, and ACAT activity is determined as described above [1]. |
| In vitro | NB-598 (10 μM) inhibits the synthesis of sterol and sterol ester from [14C]acetate without affecting the synthesis of other lipids such as phospholipids (PL), free fatty acids (FFA) and triacylglycerol (TG). In the absence of exogenous liposomal cholesterol, NB-598 reduces ACAT activity by 31%. NB-598 reduces ACAT activity by 22% even in the presence of a 600 pM concentration of liposomal cholesterol [1]. NB598 (10 μM) causes a 36±7% reduction in the total cholesterol level of MIN6 cells. NB598 causes a significant decrease in cholesterol by 49±2%, 46±7%, and 48±2% from PM, ER, and SG, respectively. NB598 dose-dependently inhibits insulin secretion under both basal (1 mM glucose) and glucose-stimulated (16.7 mM glucose) conditions. NB598 at concentrations up to 10 μM does not affect peak outward KV currents or the voltage dependence of activation but increases current inactivation [2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 10 mg/mL (22.24 mM), Sonication is recommended.
10% DMSO+90% Corn Oil : 1 mg/mL (2.22 mM), Sonication is recommended.
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| Keywords | Squalene epoxidase | NB-598 | NB598 | NB 598 | Inhibitor | inhibit |
| Inhibitors Related | Calcium Propionate | Dehydroacetic acid sodium | Potassium gluconate | D-Gluconic acid (solution) (50% in H2O) | Acetaminophen | Sulfacetamide sodium | Benzyl propionate | Terbinafine hydrochloride | Sodium formate | Magnesium acetate tetrahydrate | Geraniol | Trometamol |
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