PDK4-IN-1 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 有效抑制细胞转化和细胞增殖并诱导细胞凋亡 (
apoptosis)。PDK4-IN-1 具有抗糖尿病，抗癌和抗过敏作用。
| 生物活性 |
PDK4-IN-1 is an anthraquinone derivative and a potent and orally activepyruvate dehydrogenase kinase 4 (PDK4)inhibitor with anIC50value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and inducesapoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity[1].
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| IC50& Target |
IC50: 84 nM (Pyruvate dehydrogenase kinase 4 (PDK4))[1]
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体外研究
(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[1].
PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis[1].
PDK4-IN-1 (Compound 8c; 10 μM; 24 hours; HEK293T cells) treatment inhibits phosphorylation of Ser232, Ser293, and Ser300of PDHE1α[1].
10 μM of PDK4-IN-1 (Compound 8c) significantly increases p-Akt in AML12 cells[1].
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[1].
Cell Viability Assay[1]
| Cell 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 Analysis[1]
| Cell Line: |
HCT116 and RKO cells |
| Concentration: |
10 μM, 25 μM, 50 μM |
| Incubation Time: |
24 hours |
| Result: |
Dose-dependently increased apoptosis. |
Western Blot Analysis[1]
| Cell Line: |
HEK293T human embryonic kidney cells |
| Concentration: |
10 μM |
| Incubation Time: |
24 hours |
| Result: |
Inhibited phosphorylation of Ser232, Ser293, and Ser300of PDHE1α. |
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体内研究
(In Vivo) |
PDK4-IN-1 (Compound 8c; 100 mg/kg; oral administration; daily; for 1 week; 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, 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[1].
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[1].
| Animal Model: |
C57BL/6J mice (8-week old) fed with high-fat diet[1] |
| Dosage: |
100 mg/kg |
| Administration: |
Oral administration; daily; for 1 week |
| Result: |
Significantly improved glucose tolerance. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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