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Apoptozole
- Soluble in DMSO
- MF: C33H25F6N3O3
- MW: 625.56
Description
Apoptozole is an apoptosis-inducing inhibitor of Hsc70 and Hsp70 ATPase activity with reported Kd values of 0.21 μM and 0.14 μM for Hsc70 and Hsp70, respectively. It binds the ATPase domain of these chaperones and can restore mutant CFTR chloride-channel activity by promoting membrane trafficking.
Hsp70-family chaperones regulate protein folding, stress tolerance, apoptosis and trafficking of membrane proteins. Apoptozole is useful for studying chaperone-dependent apoptosis, proteostasis and CFTR rescue mechanisms.
Key Features
- Hsc70 and Hsp70 ATPase inhibitor
- Kd: 0.21 μM for Hsc70 and 0.14 μM for Hsp70
- Induces apoptosis through chaperone inhibition
- Promotes mutant CFTR membrane trafficking
Applications
- Heat-shock protein pharmacology
- Proteostasis and chaperone biology
- Apoptosis mechanism studies
- CFTR trafficking and chloride-channel assays
More Information
| Parent CAS No. | 1054543-47-3 |
|---|---|
| Chemical Name | 4-((2-(3,5-bis(trifluoromethyl)phenyl)-4,5-bis(4-methoxyphenyl)-1H-imidazol-1-yl)methyl)benzamide |
| SMILES | C(N)(=O)C1=CC=C(CN2C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)=NC(C3=CC=C(OC)C=C3)=C2C2=CC=C(OC)C=C2)C=C1 |
| MFCD | MFCD19443178 |
| 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 |
| CID | 24894064 |
| Short Description | Apoptosis modulator |
References
- H.J. Cho et al. 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, 133, 20267-20276.
- D.R. Williams et al. An apoptosis-inducing small molecule that binds to heat shock protein 70. Angew. Chem. Int. Ed. Engl. 2008, 47, 7466-7469.
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