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PU-H71 trihydrochloride
- Parent CAS: 873436-91-0
- Soluble in water
- MF: C18H21IN6O2S.3HCl
- MW: 621.75
Description
PU-H71 trihydrochloride (Zelavespib) is a potent heat shock protein 90 (Hsp90) inhibitor with a reported IC50 value of 51 nM.
Hsp90 stabilizes many oncogenic client proteins involved in growth, survival and stress responses. PU-H71 is used to induce client-protein degradation, inhibit tumor cell proliferation and probe chaperone dependency in cancer models including triple-negative breast cancer.
Key Features
- Potent Hsp90 inhibitor
- Reported IC50: 51 nM
- Promotes destabilization of Hsp90 client proteins
- Induces growth inhibition and apoptosis in cancer cell models
Applications
- Hsp90 chaperone pathway research
- Oncogenic client-protein degradation studies
- Breast cancer and TNBC cell models
- Proteostasis and stress-response assays
Note: On the request of the developers, this product is not for sale for our customers in the United States.
More Information
| Parent CAS No. | 873436-91-0 |
|---|---|
| Chemical Name | 8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9-(3-(isopropylamino)propyl)-9H-purin-6-amine trihydrochloride |
| SMILES | N1C(N)=C2N=C(SC3C(I)=CC4OCOC=4C=3)N(CCCNC(C)C)C2=NC=1.Cl.Cl.Cl |
| MFCD | MFCD18251588 |
| InChi | InChI=1S/C18H21IN6O2S.3ClH/c1-10(2)21-4-3-5-25-17-15(16(20)22-8-23-17)24-18(25)28-14-7-13-12(6-11(14)19)26-9-27-13;;;/h6-8,10,21H,3-5,9H2,1-2H3,(H2,20,22,23);3*1H |
| InChiKey | KMHRRRIFDIMTLR-UHFFFAOYSA-N |
| CID | 91826484 |
| Short Description | Hsp90 inhibitor |
References
- SK Moulick et al. Affinity-based proteomics reveal cancer-specific networks coordinated by Hsp90. Nature Chem. Biol. 2011, 7, 818–826.
- E Caldas-Lopes et al. Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models. Proc. Natl. Acad. Sci. USA 2009, 106, 8368.
- H He et al. Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90. J. Med. Chem. 2006, 49(1), 381-90.
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