| Bioactivity | SKF-34288 (3-Mercaptopicolinic acid) hydrochloride is an orally active phosphoenolpyruvate carboxykinase (PEPCK) inhibitor (Ki: 2-9 μM). SKF-34288 hydrochloride is a potent hypoglycemic agent by inhibiting glucose synthesis. SKF-34288 hydrochloride also inhibits Asn metabolism and increases amino acids and amides[1][2]. |
| Target | Ki: 2-9 μM (PEPCK) |
| Invitro | SKF-34288 hydrochloride (0.01-1 mM, 48 h) 抑制 C2C12 细胞增殖[4]。SKF-34288 hydrochloride (0.25-1 mM,0-5 天) 诱导 C2C12 细胞的肌原性分化[4]。SKF-34288 hydrochloride (0.25 或 1 mM) 降低 Pck2 和丝氨酸生物合成相关基因的 mRNA 表达[4]。 Cell Viability Assay[4] Cell Line: |
| In Vivo | SKF-34288 hydrochloride (37.5-150mg/kg, 口服) 降低饥饿大鼠的血糖[6]。SKF-34288 hydrochloride (25 mg/kg,皮下注射) 中和沙丁胺醇介导的兔子高血糖症[3]。SKF-34288 hydrochloride (30 和 300 mg/kg,腹腔注射) 降低丙酮酸诱导的大鼠血糖水平[5]。 Animal Model: |
| Name | SKF-34288 hydrochloride |
| CAS | 320386-54-7 |
| Formula | C6H6ClNO2S |
| Molar Mass | 191.64 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Balan MD, et al. Inhibition and Allosteric Regulation of Monomeric Phosphoenolpyruvate Carboxykinase by 3-Mercaptopicolinic Acid. Biochemistry. 2015 Sep 29;54(38):5878-87. [2]. Bailey KJ, et al. Nitrogen recycling from the xylem in rice leaves: dependence upon metabolism and associated changes in xylem hydraulics. J Exp Bot. 2016 Apr;67(9):2901-11. [3]. Reverte M, et al. Changes in plasma glucose and lactate evoked by alpha and beta 2-adrenoceptor stimulation in conscious fasted rabbits. Fundam Clin Pharmacol. 1991;5(8):663-76. [4]. Brearley MC, et al. The phosphoenolpyruvate carboxykinase (PEPCK) inhibitor, 3-mercaptopicolinic acid (3-MPA), induces myogenic differentiation in C2C12 cells. Sci Rep. 2020 Dec 17;10(1):22177. [5]. Ohmori H, et al. The Production of a Rat Model That Inhibits Phosphoenolpyruvate Carboxykinase (PEPCK), a Rate-Limiting Enzyme of Hepatic Gluconeogenesis. Adv Exp Med Biol. 2019;1155:113-118. [6]. DiTullio NW, et al. 3-mercaptopicolinic acid, an inhibitor of gluconeogenesis. Biochem J. 1974 Mar;138(3):387-94. |