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Apoptozole CAS: 1054543-47-3

Category: Inhibitors
Product Name: Apoptozole
Cat No: I000287
CAS No: 1054543-47-3
Synonyms: Apoptosis Activator VII
Molecular Formula: C33H25F6N3O3
Molecular Weight: 625.6
SMILES: 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
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
Solubility: DMSO: ≥ 31 mg/mL
Target: target: Hsp70 [1]
Storage: -20°C
CAS 1054543-47-3,Apoptozole
  • Description

Apoptozole is an inhibitor of heat shock protein 70 (Hsp70; 65% inhibition at 200 μM) that acts by blocking its ATPase activity.
target: Hsp70 [1]
In vitro: Apoptozole binds HSP70 but not other types of heat shock proteins and induces caspase-dependent apoptosis. Apoptozole does not affect interactions of HSP70 with ASK1, JNK, BAX, and AIF. [1] Apoptozole aggregates under aqueous conditions. [2]
In vivo: Animal studies indicate that Az treatment retards tumor growth in a xenograft mouse model without affecting mouse viability. [1]

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References

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
Abstract: 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.


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