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Apoptozole

Cat. No. M7575
Apoptozole  Structure
Size Price Availability Quantity
10mg USD 110 In stock
50mg USD 440 In stock
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Quality Control
Biological Activity

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.

Protocol
Cell Experiment
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
Concentrations 0-15 μM
Incubation time 18, 48, and 72 hr
Animal Experiment
Animal models Male nude mice
Formulation
Dosages 4 mg/kg
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 625.56
Formula C33H25F6N3O3
CAS Number 1054543-47-3
Purity >98%
Solubility 31 mg/mL in DMSO
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Apoptozole supplier, HSP, inhibitors

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