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PDK4-IN-1 hydrochloride

PDK4-IN-1 hydrochloride 是一种蒽醌衍生物，对丙酮酸脱氢酶激酶 4有抑制作用，IC50为 84 nM，具有口服活性。它抑制细胞转化和细胞增殖并诱导细胞凋亡。它具有抗过敏，抗糖尿病和抗癌作用。

CAS号

2310262-11-2

分子式

C22H20ClN3O2

主要靶点

PDK|Apoptosis

仅限科研使用

Cat No : CM05825

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Synonyms

验证数据展示

  • CAS No.: 2310262-11-2

    PDK4-IN-1 hydrochloride
    CAS#: 2310262-11-2

产品信息

PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4, IC50 value = 84 nM).

CAS号 2310262-11-2
分子式 C22H20ClN3O2
主要靶点 PDK|Apoptosis
主要通路 PI3K/Akt/mTOR信号通路|凋亡
分子量 393.87
纯度 ， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

Pyruvate dehydrogenase kinase 4 (PDK4):84 nM

体内活性

PDK4-IN-1 (C57BL/6J mice) treatment significantly improves glucose tolerance[1]. Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs,

体外活性

PDK4-IN-1 hydrochloride treatment significantly impedes the proliferation of human colon cancer cell lines, HCT116 and RKO. The colony formation efficiency in HCT116 and RKO cells Is significantly reduced after treatment of PDK4-IN-1[1]. PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis. PDK4-IN-1 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1[1].

溶解度

DMSO:125 mg/mL (317.36 mM),Sonification is recommended.

参考文献

1.Lee D, et al. Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases. J Med Chem. 2019 Jan 24;62(2):575-588.

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