Apoptozole
Based on 13 publication(s) in Google Scholar
Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
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- Reinheit: 99.71%
- CAS. Nr.: 1054543-47-3
- Formel: C33H25F6N3O3
- Molecular Weight:625.56
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) Apoptozole
More- Redox Biol. 2024 Apr:70:103035. [Abstract]
- Theranostics. 2021 Feb 20;11(9):4187-4206. [Abstract]
- Cell Rep Phys Sci. 2025 Jun 18;6(6).
- CNS Neurosci Ther. 2025 Mar;31(3):e70354. [Abstract]
- CNS Neurosci Ther. 2019 Sep;25(9):1030-1041. [Abstract]
- Mol Med Rep. 2025 Jun;31(6):156. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Jun;1870(5):167137. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2025 May 12;1872(6):119988. [Abstract]
- J Virol. 2025 Mar 31:e0016825. [Abstract]
- Microbiol Spectr. 2022 Feb 23;10(1):e0186021. [Abstract]
- mSphere. 2023 Apr 20;8(2):e0067922. [Abstract]
- Exp Cell Res. 2023 Mar 22;426(2):113565. [Abstract]
- Chem Asian J. 2024 Sep 2:e202400824. [Abstract]
Customer Validation & Images
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Flow Cytometry
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Cell Proliferation/Viability Assay
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Biologische Aktivität
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HSP70 0.14 μM (Kd) |
HSC70 0.21 μM (Kd) |
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 (Apoptosis Activator VII; 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[1]. 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[2]. 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[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1054543-47-3
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Appearance Solid
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Molecular Weight 625.56
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Formel C33H25F6N3O3
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Color White to off-white
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SMILES
NC(C(C=C1)=CC=C1CN2C(C3=CC=C(OC)C=C3)=C(C4=CC=C(OC)C=C4)N=C2C5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5)=O
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Synonyms
Apoptosis Activator VII
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Redox Biol
DNAJC12 causes breast cancer chemotherapy resistance by repressing doxorubicin-induced ferroptosis and apoptosis via activation of AKT. [Abstract]2024 Apr:70:103035. PMID: 38306757 -
Theranostics
SARM1 promotes neuroinflammation and inhibits neural regeneration after spinal cord injury through NF-κB signaling. [Abstract]2021 Feb 20;11(9):4187-4206. PMID: 33754056
Apoptozole purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Feb 20;11(9):4187-4206. [Abstract]
Western blot analysis of the expression of Hspa1a and NF-κB in the uninjured spinal cords from SARM1Nestin-CKO mice or injured spinal cords at 3 d after SCI from control or Apoptozole (4 mg/kg. i.p.) treated SARM1Nestin-CKO mice.
Apoptozole purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Feb 20;11(9):4187-4206. [Abstract]
HE staining images showing the inflammatory infiltration of the uninjured spinal cords from SARM1Nestin-CKO mice or injured spinal cords at 3 d after SCI from control or Apoptozole (4 mg/kg, i.p.) treated SARM1Nestin-CKO mice.
Apoptozole purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Feb 20;11(9):4187-4206. [Abstract]
Immunostaining analysis of Iba1 (green) in the uninjured spinal cords from SARM1Nestin-CKO mice or injured spinal cords at 3 d after SCI from control or Apoptozole (4 mg/kg, i.p.) treated SARM1Nestin-CKO mice.
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CNS Neurosci Ther
TSG-6 Protects Against Cerebral Ischemia-Reperfusion Injury via Upregulating Hsp70-1B in Astrocytes. [Abstract]2025 Mar;31(3):e70354. PMID: 40130432
Apoptozole purchased from MedChemExpress. Usage Cited in: CNS Neurosci Ther. 2025 Mar;31(3):e70354. [Abstract]
Astrocyte apoptosis was measured by flow cytometry treated with Apoptozole (Az).
Apoptozole purchased from MedChemExpress. Usage Cited in: CNS Neurosci Ther. 2025 Mar;31(3):e70354. [Abstract]
Astrocyte viability was determined by MTS assay at 24 h following OGD/R treated with Apoptozole (Az) (5, 10, 15 μM).
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CNS Neurosci Ther
L-glutamine protects mouse brain from ischemic injury via up-regulating heat shock protein 70. [Abstract]2019 Sep;25(9):1030-1041. PMID: 31218845 -
Mol Med Rep
2025 Jun;31(6):156. PMID: 40211707 -
Biochim Biophys Acta Mol Basis Dis
Hippocampal HDAC6 promotes POCD by regulating NLRP3-induced microglia pyroptosis via HSP90/HSP70 in aged mice. [Abstract]2024 Jun;1870(5):167137. PMID: 38527593 -
Biochim Biophys Acta Mol Cell Res
GPX4 degradation contributes to heat stress-induced liver injury via chaperone-mediated autophagy. [Abstract]2025 May 12;1872(6):119988. PMID: 40368268 -
J Virol
Heat shock protein A1 inhibits the replication of foot-and-mouth disease virus by degrading viral RNA polymerase 3D through chaperone-mediated autophagy. [Abstract]2025 Mar 31:e0016825. PMID: 40162788 -
Microbiol Spectr
Heat Shock Protein Member 8 (HSPA8) Is Involved in Porcine Reproductive and Respiratory Syndrome Virus Attachment and Internalization. [Abstract]2022 Feb 23;10(1):e0186021. PMID: 35138165 -
mSphere
Heat Shock Protein Inhibitors Show Synergistic Antibacterial Effects with Photodynamic Therapy on Caries-Related Streptococci In Vitro and In Vivo. [Abstract]2023 Apr 20;8(2):e0067922. PMID: 36853046 -
Exp Cell Res
Colorectal cancer-derived extracellular vesicles containing HSP70 enhance macrophage phagocytosis by up-regulating MARCO expression. [Abstract]2023 Mar 22;426(2):113565. PMID: 36958650 -
Chem Asian J
Selective Protein Degradation through Tetrazine Ligation of Genetically Incorporated Unnatural Amino Acids. [Abstract]2024 Sep 2:e202400824. PMID: 39221720
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (159.86 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.00 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Stock solutions of malachite green (0.081% w/v), polyvinyl alcohol (2.3% w/v), and ammonium heptamolybdate tetrahydrate (5.7% w/v in 6 M HCl) are prepared and stored at 4°C. Three solutions are mixed with water in the ratio of 2 : 1 : 1 : 2 to prepare the malachite green reagent. For the determination of the ATPase activity of Hsc70, a master mixture of an ATPase domain of Hsc70 is prepared in assay buffer (100 mM Tris-HCl, 20 mM KCl, and 6 mM MgCl2, pH 7.4) as the final concentration of 1 mM. An aliquot (10 mL) of this mixture is added into each well of a 96-well plate. To this solution is added each compound (including Apoptozole) in assay buffer, and the plate is incubated for 30 min at room temperature. To start the reaction, 1 mL of 4 mM ATP is added to the solution. The final concentrations are 1 mM protein and 200 mM ATP in 20 mL of assay buffer. After 3 h incubation at 37°C, 80 mL of the malachite green reagent is added into each well. The samples are mixed thoroughly and incubated at 37°C for 15 min, and 10 mL of 34% sodium citrate is added to stop the nonenzymatic hydrolysis of ATP. The absorbance is determined at 620 nm on a SpectraMax 340 PC 384[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male nude mice are housed in a pathogen-free room under controlled temperature and humidity. Mice aged 4 weeks are injected with tumor cells for the xenograft experiments. Viable A549 and RKO cells (5 × 106) and HeLa cells (5 × 106) are injected subcutaneously into the flank of mice. The A549 and RKO cell xenograft mice are immediately and randomly assigned to two groups. The first group (n = 10) is used as a control group and receives vehicle only. The second group (n = 10) receives intraperitoneal injections of Apoptozole (4 mg/kg/day) every other day for 2 weeks. The HeLa cell xenograft mice are immediately and randomly assigned to four groups. The first group (n = 10) is a control group receiving vehicle only. The second group (n = 10) receives intraperitoneal injections of Apoptozole (4 mg/kg/day) every other day for 2 weeks. The third group (n = 10) receives intraperitoneal injections of doxorubicin (15 mg/kg/day) every other day for 2 weeks. The fourth group (n = 10) receives intraperitoneal injections of Apoptozole (4 mg/kg/day) and doxorubicin (15 mg/kg/day) every other day for 2 weeks. Tumors in all mice are measured in two dimensions with calipers every 3 days and tumor volumes are 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 are plotted as average tumor volumes versus time[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (287 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Williams DR, et al. An apoptosis-inducing small molecule that binds to heat shock protein 70. Angew Chem Int Ed Engl. 2008;47(39):7466-9. [Content Brief]
[2]. Cho HJ, et al. Probing the effect of an inhibitor of an ATPase domain of Hsc70 on clathrin-mediated endocytosis. Mol Biosyst. 2015 Oct;11(10):2763-9. [Content Brief]
[3]. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5986 mL | 7.9928 mL | 15.9857 mL | 39.9642 mL |
| 5 mM | 0.3197 mL | 1.5986 mL | 3.1971 mL | 7.9928 mL | |
| 10 mM | 0.1599 mL | 0.7993 mL | 1.5986 mL | 3.9964 mL | |
| 15 mM | 0.1066 mL | 0.5329 mL | 1.0657 mL | 2.6643 mL | |
| 20 mM | 0.0799 mL | 0.3996 mL | 0.7993 mL | 1.9982 mL | |
| 25 mM | 0.0639 mL | 0.3197 mL | 0.6394 mL | 1.5986 mL | |
| 30 mM | 0.0533 mL | 0.2664 mL | 0.5329 mL | 1.3321 mL | |
| 40 mM | 0.0400 mL | 0.1998 mL | 0.3996 mL | 0.9991 mL | |
| 50 mM | 0.0320 mL | 0.1599 mL | 0.3197 mL | 0.7993 mL | |
| 60 mM | 0.0266 mL | 0.1332 mL | 0.2664 mL | 0.6661 mL | |
| 80 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4996 mL | |
| 100 mM | 0.0160 mL | 0.0799 mL | 0.1599 mL | 0.3996 mL |
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