计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC 50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis . PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity
In Vitro
PDK4-IN-1 (Compound 8c; 50 μM; 0-72 hours; HCT116 and RKO cells) 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. PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis. PDK4-IN-1 (Compound 8c; 10 μM; 24 hours; HEK293T cells) treatment inhibits phosphorylation of Ser 232 , Ser 293 , and Ser 300 of PDHE1α. 10 μM of PDK4-IN-1 (Compound 8c) significantly increases p-Akt in AML12 cells. PDK4-IN-1 (compound 8c)-induced phosphorylation of p53 on serine 15 is a dose-dependent response in both HCT116 and RKO cells. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HCT116 and RKO cells Concentration: 50 μM Incubation Time: 0 hour, 24 hours, 48 hours, 72hours Result: Significantly impeded the proliferation of human colon cancer cell lines, HCT116 and RKO. Apoptosis AnalysisCell Line: HCT116 and RKO cells Concentration: 10 μM, 25 μM, 50 μM Incubation Time: 24 hours Result: Dose-dependently increased apoptosis. Western Blot AnalysisCell Line: HEK293T human embryonic kidney cells Concentration: 10 μM Incubation Time: 24 hours Result: Inhibited phosphorylation of Ser 232 , Ser 293 , and Ser 300 of PDHE1α.
In Vivo
PDK4-IN-1 (Compound 8c; 100 mg/kg; oral administration; daily; for 1 week; C57BL/6J mice) treatment significantly improves glucose tolerance . Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs, showing that the absorbance values are 0.26, 0.20, and 0.126 in IgE/Ag, 10 μM, and 20 μM PDK4-IN-1-treated BMMCs . The pharmacokinetic (PK) profiles of PDK4-IN-1 (compound 8c) are evaluated in rat. PDK4-IN-1 shows good bioavailability (64%), long half-life (>7 h), and moderate clearance (CL of 0.69) in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6J mice (8-week old) fed with high-fat diet Dosage: 100 mg/kg Administration: Oral administration; daily; for 1 week Result: Significantly improved glucose tolerance.
IC50& Target:IC50: 84 nM (Pyruvate dehydrogenase kinase 4 (PDK4))
规格
别名
PDK4-IN-1盐酸盐
规格或纯度
10mM in DMSO
英文名称
PDK4-IN-1 hydrochloride
生化机理
PDK4-IN-1 盐酸盐是一种蒽醌衍生物，也是一种强效口服活性丙酮酸脱氢酶激酶 4（PDK4）抑制剂，IC 50 值为 84 nM。PDK4-IN-1 盐酸盐能有效抑制细胞转化和细胞增殖。
储存条件
干燥,-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CNCCC1N2C=C(C=N2)C3=C4C(=CC=C3)C(=O)C5=CC=CC=C5C4=O.Cl
关联CAS
分子量
393.87
技术文档
高级数据
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C、干燥条件下保存。请与干燥剂一同密封保存，本品对湿气敏感。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2310262-11-2，分子式为 C22H20ClN3O2，分子量为 393.87 g/mol。
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