PS10

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PS10

CAS No. : 1564265-82-2

MCE 国际站：PS10

产品活性：PS10 是一种新型，有效且具有 ATP 竞争性的广谱 PDK 抑制剂，可抑制所有 PDK 同工型，对 PDK2，PDK4，PDK1 和 PDK3 的 IC₅₀ 分别为 0.8 μM，0.76 μM，2.1 μM 和 21.3 μM。 PS10 对 PDK2 (K_d= 239 nM) 的亲和力高于对 Hsp90 (K_d= 47 μM)。 PS10 改善葡萄糖耐量，刺激饮食引起的肥胖症中的心肌碳水化合物氧化。 PS10 具有研究糖尿病性心肌病的潜力。

研究领域：Metabolic Enzyme/Protease

作用靶点：PDHK

In Vitro: PS10 shows a higher affinity of PS10 for PDK2 (K_d= 239 nM) than for Hsp90 (K_d= 47,000 nM).
PS10 is less potent than cycloheximide in HeLa cells, it shows an IC₅₀ value of 284 μM for the growth inhibition and PS10 has low toxicity in cells.

In Vivo: PS10 (Intraperitoneal injection; 70 mg/kg; single dose) treatment lead to 11- and 23-fold higher PDC activity in heart and liver, respectively. Meanwhile, there results in a 1.4-fold enhancement of PDC activity in kidneys compared with vehicle-group.
PS10 (Intraperitoneal injection; 70 mg/kg; 3 days) treatment results that thePDC activity profiles and the phospho-E1α subunit level is similar to the single-dose. Notably, the three-day treatment attenuates the enhancement of PDK activity in heart.
PS10 (intraperitoneal injection; 70 mg/kg; 4 weeks) is treated in mice and subjected to a glucose tolerance test. when challenged with 1.5 g/kg glucose, the plasma glucose level in the vehicle-treated control is at 200 mg/dl at 0 min, peaks at 482 mg/dl at 30 min, and reduces to 210 mg/dl at 120 min. In PS10-treated DIO mice, the glucose level at 168 mg/dl at 0 min is lower than that in vehicle-treated animals, reachs 312 mg/dl at 30 min, and returns to 163 mg/dl at 120 min.
PS10 (intraperitoneal injection; 70 mg/kg) and DCA both stimulates flux through PDC as measured by the appearance of hyperpolarized [¹³C]bicarbonate. It shows similar glucose tolerance response to glucose challenge restores PDC activity in the DIO mouse hearts.

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