PDK4-IN-1 HYDROCHLORIDE
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- CAS号:
- 2310262-11-2
- 英文名:
- PDK4-IN-1 hydrochloride
- 英文别名:
- PDK4-IN-1 hydrochloride;1-(1-(Piperidin-4-yl)-1H-pyrazol-4-yl)anthracene-9,10-dione hydrochloride;inhibit,anti-allergic,Pyruvate dehydrogenase kinase,PDHE1α,antidiabetic,p53,BCL-xL,PARP1,caspase-3,BAX,Inhibitor,p-Akt,Apoptosis,PDK4,PDK4 IN 1 hydrochloride,PDK4IN1 hydrochloride,PDK-4-IN-1 hydrochloride,PDHK,metabolites,PDH kinase,anticancer
- 中文名:
- PDK4-IN-1 HYDROCHLORIDE
- 中文别名:
- 化合物 T12412L;PDK4-IN-1 HYDROCHLORIDE;化合物PDK4-IN-1? HYDROCHLORIDE;1-(1-(哌啶-4-基)-1H-吡唑-4-基)蒽-9,10-二酮盐酸盐
- CBNumber:
- CB98044775
- 分子式:
- C22H20ClN3O2
- 分子量:
- 393.87
- MOL File:
- 2310262-11-2.mol
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PDK4-IN-1 HYDROCHLORIDE化学性质
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储存条件:
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Inert atmosphere,Room Temperature
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溶解度:
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DMSO: 125 mg/mL (317.36 mM)
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PDK4-IN-1 HYDROCHLORIDE性质、用途与生产工艺
PDK4-IN-1 hydrochloride 是一种蒽醌衍生物，也是一种有效的，口服活性的丙酮酸脱氢酶激酶 4 (PDK4) 抑制剂，IC50 值为 84 nM。PDK4-IN-1 hydrochloride 有效抑制细胞转化和细胞增殖并诱导细胞凋亡 (apoptosis)。PDK4-IN-1 hydrochloride 具有抗糖尿病，抗癌和抗过敏作用。
IC50: 84 nM (Pyruvate dehydrogenase kinase 4 (PDK4))
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.
Cell Viability Assay
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Cell Line:
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HCT116 and RKO cells
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Concentration:
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50 μM
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Incubation Time:
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0 hour, 24 hours, 48 hours, 72hours
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Result:
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Significantly impeded the proliferation of human colon cancer cell lines, HCT116 and RKO.
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Apoptosis Analysis
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Cell Line:
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HCT116 and RKO cells
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Concentration:
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10 μM, 25 μM, 50 μM
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Incubation Time:
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24 hours
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Result:
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Dose-dependently increased apoptosis.
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Western Blot Analysis
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Cell Line:
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HEK293T human embryonic kidney cells
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Concentration:
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10 μM
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Incubation Time:
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24 hours
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Result:
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Inhibited phosphorylation of Ser
232
, Ser
293
, and Ser
300
of PDHE1α.
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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.
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Animal Model:
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C57BL/6J mice (8-week old) fed with high-fat diet
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Dosage:
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100 mg/kg
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Administration:
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Oral administration; daily; for 1 week
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Result:
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Significantly improved glucose tolerance.
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PDK4-IN-1 HYDROCHLORIDE
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-135954A | PDK4-IN-1 hydrochloride | | 1 mg | 1727元 |
| 2024/04/30 | HY-135954A | PDK4-IN-1 HYDROCHLORIDE
PDK4-IN-1 hydrochloride | 2310262-11-2 | 10mM * 1mLin DMSO | 4180元 |
PDK4-IN-1 HYDROCHLORIDE
生产厂家
2310262-11-2, PDK4-IN-1 HYDROCHLORIDE 相关搜索:
- 化合物PDK4-IN-1? HYDROCHLORIDE
- 化合物 T12412L
- 1-(1-(哌啶-4-基)-1H-吡唑-4-基)蒽-9,10-二酮盐酸盐
- PDK4-IN-1 HYDROCHLORIDE
- 2310262-11-2
- inhibit,anti-allergic,Pyruvate dehydrogenase kinase,PDHE1α,antidiabetic,p53,BCL-xL,PARP1,caspase-3,BAX,Inhibitor,p-Akt,Apoptosis,PDK4,PDK4 IN 1 hydrochloride,PDK4IN1 hydrochloride,PDK-4-IN-1 hydrochloride,PDHK,metabolites,PDH kinase,anticancer
- 1-(1-(Piperidin-4-yl)-1H-pyrazol-4-yl)anthracene-9,10-dione hydrochloride
- PDK4-IN-1 hydrochloride