MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

PS10

CAS No. : 1564265-82-2

MCE 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.

相关产品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  Metabolism/Protease Compound Library  |  Diabetes Related Compound Library  |  Glycolysis Compound Library  |  Sodium dichloroacetate  |  VER-246608  |  AZD7545  |  Dicoumarol  |  JX06  |  M77976  |  PDK4-IN-1 hydrochloride

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。