Hsp90-Cdc37-IN-3

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Hsp90-Cdc37-IN-3 

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)。

Hsp90-Cdc37-IN-3

Hsp90-Cdc37-IN-3 Chemical Structure

CAS No. : 2361009-68-7

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生物活性

Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis[1].

IC50 & Target

Hsp90-Cdc37

 

体外研究
(In Vitro)

Hsp90-Cdc37-IN-3 (Compound 9) (24 h) shows broad-spectrum antitumor potential with IC50 values 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/G1 phase in a dose-dependent manner[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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/G1 phase in a dose-dependent manner.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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*107 in 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.

分子量

638.19

Formula

C35H44ClN3O6
CAS 号

2361009-68-7
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.
参考文献

  • [1]. Na Li, et al. Discovery of Novel Celastrol-Imidazole Derivatives with Anticancer Activity In Vitro and In Vivo. J Med Chem. 2022 Mar 24;65(6):4578-4589.

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