For research use only. Not for therapeutic Use.
Apoptozole (Cat No.:I000287) is a small molecule inhibitor that targets heat shock protein 70 (Hsp70) and inhibits its anti-apoptotic functions. It has been shown to induce apoptosis in cancer cells and enhance the cytotoxic effects of chemotherapy drugs. Apoptozole binds to the ATP-binding domain of Hsp70, disrupting its interaction with pro-apoptotic proteins and promoting cell death. It has demonstrated efficacy in preclinical studies as a potential therapeutic agent for cancer treatment. Further research is ongoing to explore its therapeutic applications and potential clinical use.
| Catalog Number | I000287 |
| CAS Number | 1054543-47-3 |
| Synonyms | Apoptosis Activator VII |
| Molecular Formula | C33H25F6N3O3 |
| Purity | ≥95% |
| Target | Metabolic Enzyme/Protease |
| Solubility | DMSO: ≥ 31 mg/mL |
| Storage | -20°C |
| IUPAC Name | 4-[[2-[3,5-bis(trifluoromethyl)phenyl]-4,5-bis(4-methoxyphenyl)imidazol-1-yl]methyl]benzamide |
| InChI | InChI=1S/C33H25F6N3O3/c1-44-26-11-7-20(8-12-26)28-29(21-9-13-27(45-2)14-10-21)42(18-19-3-5-22(6-4-19)30(40)43)31(41-28)23-15-24(32(34,35)36)17-25(16-23)33(37,38)39/h3-17H,18H2,1-2H3,(H2,40,43) |
| InChIKey | ZIMMTPFXOMAJTQ-UHFFFAOYSA-N |
| SMILES | COC1=CC=C(C=C1)C2=C(N(C(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)CC4=CC=C(C=C4)C(=O)N)C5=CC=C(C=C5)OC |
| Reference | 1:PLoS One. 2015 Oct 12;10(10):e0140006. doi: 10.1371/journal.pone.0140006. eCollection 2015. Investigating Apoptozole as a Chemical Probe for HSP70 Inhibition.Evans LE,Cheeseman MD,Yahya N,Jones K, PMID: 26458144 PMCID: PMC4601772 DOI: 10.1371/journal.pone.0140006 </br><span>Abstract:</span> The use of chemical tools to validate clinical targets has gained in popularity over recent years and the importance of understanding the activity, selectivity and mechanism of action of these compounds is well recognized. Dysregulation of the HSP70 protein family has been linked to multiple cancer types and drug resistance, highlighting their importance as popular targets for anti-cancer drug development. Apoptozole is a recently identified small molecule, which has been reported to possess strong affinity for the HSP70 isoforms HSP72 and HSC70. We investigated apoptozole as a potential chemical tool for HSP70 inhibition. Unfortunately, using both biochemical and biophysical techniques, we were unable to find any experimental evidence that apoptozole binds to HSP70 in a specific and developable way. Instead, we provide experimental evidence that apoptozole forms aggregates under aqueous conditions that could interact with HSP70 proteins in a non-specific manner. |
