In vitro: Apoptozole is an inhibitor of Hsc70 and Hsp70, which binds to Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively. Apoptozole (1 μM) induces apoptosis in P19 cells. Apoptozole shows inhibitory activities against several cancer cell lines, such as SK-OV-3 (ovarian cancer cells), HCT-15 (colon cancer cells), and A549 (lung cancer cells), with IC50s of 0.22, 0.25, and 0.13 μM, respectively. Apoptozole binds to the ATPase domain of Hsc70 and Hsp70, but does not binds to other types of heat shock proteins such as Hsp60, Hsp90 or Hsp40. Apoptozole (0-15 μM) suppresses the growth of A549 cells, HeLa cells, and MDA-MB-231 cells, with IC50s ranging from 5 to 7 μM. Apoptozole (5 or 10 μM) shows no effect on associations of HSP70 with ASK1, JNK, or BAX, and does not induce AIF-mediated caspase-independent apoptosis in HeLa cells.
In vivo: Apoptozole (4 mg/kg, i.p.) exhibits antitumor activities in nude mice xenografted with A549, RKO (colorectal carcinoma), and HeLa cells.
|Cell lines||A549 and RKO cells|
|Preparation method||Cells (5 × 105 per well) are plated in triplicate in 96-well plates in 0.1 mL of culture media with 10% FBS. After 24 hr, cells are treated with various concentrations of Apoptozole (0-15 μM) in culture media with 3% FBS (final volume: 0.2 mL per well) for 18, 48, and 72 hr before treatment with MTT. Absorbance at 570 nm is measured using a UV microplate reader|
|Incubation time||18, 48, and 72 hr|
|Animal models||Male nude mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||31 mg/mL in DMSO|
Anti-leukemia activity of a Hsp70 inhibitor and its hybrid molecules.
Park SH, et al. Sci Rep. 2017 Jun 14;7(1):3537. PMID: 28615625.
A small molecule inhibitor for ATPase activity of Hsp70 and Hsc70 enhances the immune response to protein antigens.
Baek KH, et al. Sci Rep. 2015 Dec 3;5:17642. PMID: 26631605.
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