| Identification | Back Directory | [Name]
[1,1'-Biphenyl]-3-carboxamide, N-[7-(acetyloxy)-8-methoxy-2-oxo-2H-1-benzopyran-3-yl]-3',6-dimethoxy- | [CAS]
1160952-43-1 | [Synonyms]
KU-177
[1,1'-Biphenyl]-3-carboxamide, N-[7-(acetyloxy)-8-methoxy-2-oxo-2H-1-benzopyran-3-yl]-3',6-dimethoxy- | [Molecular Formula]
C27H23NO8 | [MOL File]
1160952-43-1.mol | [Molecular Weight]
489.47 |
| Hazard Information | Back Directory | [Uses]
KU-177 is a potent inhibitor of Hsp90 ATPase homologue 1 (Aha1), ablates Aha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disrupts Aha1/Hsp90 interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research[1][2]. | [in vivo]
KU-177 (1 mg/kg; i.p.; twice a week; 4 weeks), inhibits tumor growth and extends the survival of 5TMM3VT MM mice without significant toxicity. KU-177 shows stronger efficacy in vivo, combined with Bortezomib.html" class="link-product" target="_blank">Bortezomib (HY-10227) (1 mg/kg; i.p.)[1].
| Animal Model: | 5TMM3VT mouse model (6-8 weeks old, C57BL/KaLwrij mice)[1] | | Dosage: | 1 mg/kg | | Administration: | Intraperitoneal injection; twice a week; sacrificed mice with hindlimb weakness immediately, about 4-5 weeks | | Result: | Inhibited the xenograft tumor growth of both ANBL6 WT/BTZ-DR cells.
Didn’t induce histopathological abnormities or lesions in main organs including heart, liver, spleen, lung and kidney. |
| [IC 50]
HSP90 | [References]
[1] Gu C, et al. AHSA1 is a promising therapeutic target for cellular proliferation and proteasome inhibitor resistance in multiple myeloma. J Exp Clin Cancer Res. 2022 Jan 6;41(1):11. DOI:10.1186/s13046-021-02220-1
[2] Keegan BM, et al. Synthesis and Evaluation of Small Molecule Disruptors of the Aha1/Hsp90 Complex for the Reduction of Tau Aggregation. ACS Med Chem Lett. 2022 Apr 15;13(5):827-832. DOI:10.1021/acsmedchemlett.2c00064 |
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