Apoptozole
Apoptozole, also known as Apoptosis Activator VII, is a selective inhibitor of heat shock protein 70 (Hsp70; 65% inhibition at 200 µM) that acts by blocking its ATPase activity. Apoptozole enhances immune responses to administered antigens. Treatment of mice with Apoptozole elicits production of antibodies with a high IgG2c/IgG1 ratio and stimulates the release of Th1 and Th2-type cytokines, suggesting that Apoptozole activates the Th1 and Th2 immune responses. The ATPase activities of Hsp70 and Hsc70 are known to be responsible for regulation of various biological processes.
1: Roundhill E, Turnbull D, Burchill S. Localization of MRP-1 to the outer mitochondrial membrane by the chaperone protein HSP90β. FASEB J. 2016 May;30(5):1712-23. doi: 10.1096/fj.15-283408. PubMed PMID: 26722004.
2: Baek KH, Zhang H, Lee BR, Kwon YG, Ha SJ, Shin I. A small molecule inhibitor for ATPase activity of Hsp70 and Hsc70 enhances the immune response to protein antigens. Sci Rep. 2015 Dec 3;5:17642. doi: 10.1038/srep17642. PubMed PMID: 26631605; PubMed Central PMCID: PMC4668564.
3: Evans LE, Cheeseman MD, Yahya N, Jones K. Investigating Apoptozole as a Chemical Probe for HSP70 Inhibition. PLoS One. 2015 Oct 12;10(10):e0140006. doi: 10.1371/journal.pone.0140006. PubMed PMID: 26458144; PubMed Central PMCID: PMC4601772.
4: Ko SK, Kim J, Na DC, Park S, Park SH, Hyun JY, Baek KH, Kim ND, Kim NK, Park YN, Song K, Shin I. A small molecule inhibitor of ATPase activity of HSP70 induces apoptosis and has antitumor activities. Chem Biol. 2015 Mar 19;22(3):391-403. doi: 10.1016/j.chembiol.2015.02.004. PubMed PMID: 25772468.
5: Cho HJ, Kim GH, Park SH, Hyun JY, Kim NK, Shin I. Probing the effect of an inhibitor of an ATPase domain of Hsc70 on clathrin-mediated endocytosis. Mol Biosyst. 2015 Oct;11(10):2763-9. doi: 10.1039/c4mb00695j. PubMed PMID: 25728281.
6: Cho HJ, Gee HY, Baek KH, Ko SK, Park JM, Lee H, Kim ND, Lee MG, Shin I. A small molecule that binds to an ATPase domain of Hsc70 promotes membrane trafficking of mutant cystic fibrosis transmembrane conductance regulator. J Am Chem Soc. 2011 Dec 21;133(50):20267-76. doi: 10.1021/ja206762p. PubMed PMID: 22074182.
2: Baek KH, Zhang H, Lee BR, Kwon YG, Ha SJ, Shin I. A small molecule inhibitor for ATPase activity of Hsp70 and Hsc70 enhances the immune response to protein antigens. Sci Rep. 2015 Dec 3;5:17642. doi: 10.1038/srep17642. PubMed PMID: 26631605; PubMed Central PMCID: PMC4668564.
3: Evans LE, Cheeseman MD, Yahya N, Jones K. Investigating Apoptozole as a Chemical Probe for HSP70 Inhibition. PLoS One. 2015 Oct 12;10(10):e0140006. doi: 10.1371/journal.pone.0140006. PubMed PMID: 26458144; PubMed Central PMCID: PMC4601772.
4: Ko SK, Kim J, Na DC, Park S, Park SH, Hyun JY, Baek KH, Kim ND, Kim NK, Park YN, Song K, Shin I. A small molecule inhibitor of ATPase activity of HSP70 induces apoptosis and has antitumor activities. Chem Biol. 2015 Mar 19;22(3):391-403. doi: 10.1016/j.chembiol.2015.02.004. PubMed PMID: 25772468.
5: Cho HJ, Kim GH, Park SH, Hyun JY, Kim NK, Shin I. Probing the effect of an inhibitor of an ATPase domain of Hsc70 on clathrin-mediated endocytosis. Mol Biosyst. 2015 Oct;11(10):2763-9. doi: 10.1039/c4mb00695j. PubMed PMID: 25728281.
6: Cho HJ, Gee HY, Baek KH, Ko SK, Park JM, Lee H, Kim ND, Lee MG, Shin I. A small molecule that binds to an ATPase domain of Hsc70 promotes membrane trafficking of mutant cystic fibrosis transmembrane conductance regulator. J Am Chem Soc. 2011 Dec 21;133(50):20267-76. doi: 10.1021/ja206762p. PubMed PMID: 22074182.
| Chemical | |
|---|---|
| CAS Num | 1054543-47-3 |
| Chemical Formula | C33H25F6N3O3 |
| Molecular Weight | 625.5714 |
| IUPAC Chemical Name | 4-((2-(3,5-bis(trifluoromethyl)phenyl)-4,5-bis(4-methoxyphenyl)-1H-imidazol-1-yl)methyl)benzamide |
| Exact Mass | 625.18 |
| Elemental Analysis | C, 63.36; H, 4.03; F, 18.22; N, 6.72; O, 7.67 |
| Synonym | Apoptozole; Apoptosis Activator VII. |
| Solubility | Soluble in DMSO |
| SMILES Code | COC(C=C1)=CC=C1C2=C(C3=CC=C(OC)C=C3)N(CC4=CC=C(C(N)=O)C=C4)C(C5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5)=N2 |
| Biological | |
| Targets and Effects | Hsp70 |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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