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Apoptozole

Catalog No. T3293   CAS 1054543-47-3
Synonyms: Apoptosis Activator VII

Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, and can induce apoptosis.

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Apoptozole Chemical Structure
Apoptozole, CAS 1054543-47-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 30.00
5 mg In stock $ 43.00
10 mg In stock $ 76.00
25 mg In stock $ 139.00
50 mg In stock $ 247.00
100 mg In stock $ 368.00
200 mg In stock $ 543.00
1 mL * 10 mM (in DMSO) In stock $ 60.00
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Purity: 98.02%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, and can induce apoptosis.
Targets&IC50 HSP70:0.14 μM(Kd), HSC70:0.21 μM(Kd)
In vitro Apoptozole induces caspase dependent apoptosis by blocking interaction of HSP70 with APAF-1, without affecting interactions of HSP70 with ASK1, JNK, BAX, and AIF[2]. However, apoptozole may form aggregates under aqueous conditions that could interact with HSP70 proteins in a non-specific manner, potentially leading to false positives and inconsistent data[3].
In vivo Apoptozole greatly retards tumor growth in mice xenografted with cancer cells without affecting mouse viability. The elimination half-life time (T1/2) of Az in blood is found to be significantly longer than that of Dox (8.04 versus 1.60 hr) and the time needed to reach a maximum concentration (Tmax) of Az is shorter than that of Dox (1.00 versus 4.00 hr)[2].
Kinase Assay Inhibition of HER2/erbB2 tyrosine kinase activity: BT-474 cells are seeded on 24-well plates and cultured overnight. Mubritinib is then added at various concentrations. After incubation for 2 hours, the cells are harvested directly into sodium dodecyl sulfate (SDS)-sample buffer (200 μL). Aliquots containing equal amounts of total cell extract are run on 7.5% to 15% gradient SDS–polyacrylamide gel electrophoresis (PAGE). Following electrophoresis, proteins are transferred onto a polyvinylidene fluoride (PVDF) membrane, for western blot analysis using a relevant primary antibody. Detection of protein is accomplished by an enhanced chemiluminescent (ECL) detection method. The extent of tyrosine phosphorylation of HER2/erbB2 is measured by the LAS-1000 plus lumino-image analyser. The concentration of Mubritinib that inhibits HER2/erbB2 phosphorylation by 50% (IC50) is calculated from a dose–response curve generated by least-squares linear regression of the response using SAS software.
Cell Research Several cancer cell lines (A549, lung adenocarcinoma epithelial cells; HeLa, cervical cancer cells; MDA-MB-231, breast cancer cells; HepG2, liver cancer cells) are treated with various concentrations (0-15 μM) of Az or compound 7 as a negative control for 18 hr. Cell viabilities are then determined using an MTT assay.(Only for Reference)
Synonyms Apoptosis Activator VII
Molecular Weight 625.56
Formula C33H25F6N3O3
CAS No. 1054543-47-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 24 mg/mL (38.4 mM)

DMSO: 93 mg/mL (148.7 mM)

TargetMolReferences and Literature

1. Williams DR, et al. Angew Chem Int Ed Engl. 2008, 47(39):7466-9. 2. Ko SK, et al. Chem Biol. 2015, 22(3):391-403. 3. Evans LE, et al. PLoS One. 2015, 10(10):e0140006.

Related compound libraries

This product is contained In the following compound libraries:
Endoplasmic Reticulum Stress Compound Library Anti-Metabolism Disease Compound Library Anti-Breast Cancer Compound Library Cuproptosis Compound Library Anti-COVID-19 Compound Library Apoptosis Compound Library Cytoskeletal Signaling Pathway Compound Library Fluorochemical Library Inhibitor Library Metabolism Compound Library

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Keywords

Apoptozole 1054543-47-3 Apoptosis Cytoskeletal Signaling Metabolism HSP domain Heat shock proteins inhibit Inhibitor Apoptosis Activator VII Hsp70 ATPase Hsc70 inhibitor

 

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