Hsp90-Cdc37-IN-3 (Compound 9) 是一种具有抗癌活性 (anticancer) 的新型 celastrol–imidazole 衍生物。Hsp90-Cdc37-IN-3 通过共价结合抑制Hsp90–Cdc37，诱导细胞凋亡 (apoptosis)。
| 生物活性 | Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol–imidazole derivative withanticanceractivity. Hsp90-Cdc37-IN-3 inhibitsHsp90–Cdc37by covalent-binding, and inducesapoptosis[1]. |
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体外研究
(In Vitro) | Hsp90-Cdc37-IN-3 (Compound 9) (24 h) shows broad-spectrum antitumor potential with IC50values of 0.54, 0.59, 0.57, and 0.57 μM against A549, HTC116, U2OS, and MDA-MB231 cells, respectively[1].
Hsp90-Cdc37-IN-3 (0-5 μM, 12 h) inhibits Hsp90–Cdc37 and influences the function of apoptosis-related proteins by covalently combining with both Hsp90 and Cdc37[1].
Hsp90-Cdc37-IN-3 (0-0.8 μM, 48 h) induces apoptosis significantly in A549 cells[1].
Hsp90-Cdc37-IN-3 (0-0.4 μM, 24 h) arrests the cell cycle in the G0/G1phase in a dose-dependent manner[1].
Western Blot Analysis[1] | Cell Line: | A549 | | Concentration: | 1.25, 2.5, and 5 μM | | Incubation Time: | 12 h | | Result: | Downregulated the levels of Hsp90–Cdc37 clients (p-Akt and Cdk4) in a dose-dependent manner, and the levels of apoptosis-related proteins (Bax, Bcl-2, cleaved caspase-3, and cleaved PARP) were significantly regulated. |
Apoptosis Analysis[1] | Cell Line: | A549 | | Concentration: | 0.2, 0.4, and 0.8 μM | | Incubation Time: | 48 h | | Result: | Induced apoptosis significantly. |
Cell Cycle Analysis[1] | Cell Line: | A549 | | Concentration: | 0.1, 0.2, and 0.4 μM | | Incubation Time: | 24 h | | Result: | Arrested the cell cycle in the G0/G1phase in a dose-dependent manner. |
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体内研究
(In Vivo) | Hsp90-Cdc37-IN-3 (Compound 9) (0-1 mg/kg; i.p.; once a day, 21 days) shows strong antitumor activity with no significant toxicity[1].
| Animal Model: | Female BALB/c nude mice at 6 weeks old[1]. | | Dosage: | 0.5 mg/kg or 1 mg/kg. Mice were inoculated subcutaneously with A549 cells (1*107in 100 μL of PBS for each mouse). | | Administration: | Intraperitoneal injection, once a day, 21 days | | Result: | Decreased tumor weight and enhanced TIR without show toxicity. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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