Hsp90-IN-45
Hsp90-IN-45 is a Hsp90 inhibitor. Hsp90-IN-45 competitively binds to the ATP-binding site of purified Hsp90α with a Kd of 70 nM, blocks ATP hydrolysis, and disrupts Hsp90 client signaling. Hsp90-IN-45 inhibits ATPase activity of purified Hsp90α. Hsp90-IN-45 will be radiolabeled with 76/77Br for use as a radiotheragnostic agent for PET imaging and Meitner-Auger electron therapy. Hsp90-IN-45 can be used for the research of cancer.
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- Formule: C22H26BrN3O3
- Masse moléculaire:460.36
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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HSP90α |
Hsp90-IN-45 (Compound 21) (1-32 μM; 90 min) dose-dependently inhibits the Ahsa1-stimulated ATPase activity of purified Hsp90α[1].
Hsp90-IN-45 (5-320 nM; overnight) competitively binds to the ATP-binding site of purified Hsp90α with high affinity (Kd = 70 nM)[1].
Hsp90-IN-45 (1-100 μM; 24 h) penetrates MDA-MB-231 cells, induces a heat shock response (measured by Hsp27 upregulation) at 1 and 10 μM after 24 h, and inhibits Hsp90 client protein signaling (measured by p-ERK1/2 downregulation) at 100 μM after 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 breast cancer cells
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Concentration:1, 10, 100 μM
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Incubation Time:24 h
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Result:Strongly reduced p-ERK1/2 levels at 100 μM, indicating inhibition of Hsp90 client protein signaling.
Induced a significant increase in Hsp27 levels at 1 μM and 10 μM, triggering the heat shock response at lower concentrations than those required for client signaling inhibition.
Chemical Information
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Masse moléculaire 460.36
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Formule C22H26BrN3O3
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SMILES
O=C(C1=CC(Br)=C(O)C=C1O)N(C2)CC3=C2C=CC(CN[C@@H]4CCCN(C)C4)=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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