Inhibitors, Agonists, Screening Libraries
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BIOLOGICAL ACTIVITY:
Apoptozole is an inhibitor of heat shock protein 70 (Hsp70; 65% inhibition at 200 μM) that acts by blocking its ATPase activity.target: Hsp70 [1]
电子台历In vitro: Apoptozole binds HSP70 but not other types of heat shock proteins and induces caspase–dependent apoptosis. Apoptozole does not affect interactions of HSP70 with ASK1, JNK, BAX, and AIF. [1] Apoptozole aggregates under aqueous conditions. [2]煎蛋锅
In vivo: Animal studies indicate that Az treatment retards tumor growth in a xenograft mouse model without affecting mouse viability.
[1]
PROTOCOL (Extracted from published papers and Only for reference)
抗菌
防臭袜
cell assay [1]
Cells (5 × 103 per well) were plated in triplicate in 96–well plates in 0.1 ml of culture media with 10% FBS. After 24 hr, cells werej biol chem
treated with various concentrations of Az (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. MTT assays were performed according to general procedures. Absorbance at 570 nm was measured using a UV microplate reader.
Animal administration: [1]
Male nude mice were purchased from Orient Bio Co. The animals were housed in a pathogen–free room under controlled temperature and humidity. The animal study was conducted according to the established procedures of the Yonsei University Laboratory Animal Maintenance Manual. Mice aged 4 weeks were injected with tumor cells for the xenograft experiments. Viable A549 and RKO cells (5 ×106) and HeLa cells (5 × 106) were injected subcutaneously into the flank of mice. The A549 and RKO cell xenograft mice were immediately and randomly assigned to two groups. The first group (n = 10) was used as a control group and received vehicle only.The second group (n = 10) received intraperitoneal injections of Az (4 mg/kg/day) every other day for 2 weeks. The HeLa cell xenograft mice were immediately and randomly assigned to four groups. The first group (n = 10) was a control group receiving
vehicle only. The second group (n = 10) received intraperitoneal injections of Az (4 mg/kg/day) every
other day for 2 weeks. The third group (n = 10) received intraperitoneal injections of doxorubicin (15 mg/kg/day) every other day for 2 weeks. The fourth group (n =
10) received intraperitoneal injections of Az (4 mg/kg/day) and doxorubicin (15 mg/kg/day) every other day for 2 weeks. Tumors in all mice were measured in two dimensions with calipers every 3 days and tumor volumes were calculated using the formula volume = w × l2/2, where w is the width at the widest point of the tumor and l is the length perpendicular to w. The results from individual mice were plotted as average tumor volumes ver
References:
aa187[1]. Ko SK et al. A small molecule inhibitor of ATPase activity of HSP70 induces apoptosis and has antitumor activities. Chem Biol. 2015 Mar 19;22(3):391–403.
Apoptozole Cat. No.:
HY-15098CAS No.:
1054543-47-3Molecular Formula:
C 33H 25F 6N 3O 3Molecular Weight:
625.56Target:
HSP; HSP Pathway:
Metabolic Enzyme/Protease; Cell Cycle/DNA Damage Solubility:
DMSO: ≥ 31 mg/mL
[2]. Evans LE et al. Investigating Apoptozole as a Chemical Probe for HSP70 Inhibition. PLoS One. 2015 Oct 12;10(10)
Caution: Product has not been fully validated for medical applications. For research use only.
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