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 K_d 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^[1].

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 (K_d = 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.

460.36

C₂₂H₂₆BrN₃O₃

O=C(C1=CC(Br)=C(O)C=C1O)N(C2)CC3=C2C=CC(CN[C@@H]4CCCN(C)C4)=C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Kennedy AK, et al. Novel Hsp90 inhibitors as leads for the development of radiotheragnostics for Meitner-Auger electron therapy. Bioorg Chem. 2026;170:109522.  [Content Brief]