KU-177
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.
For research use only. We do not sell to patients.
- CAS No.: 1160952-43-1
- Formula: C27H23NO8
- Molecular Weight:489.47
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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HSP90 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
8.62 μM
Compound: 12c
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Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 72 hrs by MTS/PMS assay
Antiproliferative activity against human MCF7 cells expressing estrogen receptor after 72 hrs by MTS/PMS assay
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[PMID: 21553822] |
| SK-BR-3 | IC50 |
20.5 μM
Compound: 12c
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Antiproliferative activity against human SKBR3 cells expressing HER2 after 72 hrs by MTS/PMS assay
Antiproliferative activity against human SKBR3 cells expressing HER2 after 72 hrs by MTS/PMS assay
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[PMID: 21553822] |
In Vitro
KU-177 (50 μM; 48 h) hampers the proliferation of flow MRD-positive cells in both primary multiple myeloma (MM) and recurrent MM patient samples[1].
KU-177 (30 μM; 48 h) inhibits proteasome activity in AHSA1 WT/OE cells, PSMD2 WT/OE cells and ANBL6 WT/DR cells[1].
KU-177 abrogates the cellular proliferation and PI resistance induced by elevated AHSA1, and decreases the expression of CDK6 and PSMD2[1].
KU-177 (25 μM; 30 min; 37 °C) inhibits recombinant P301L tau aggregation without inhibiting Hsp90 to refold luciferase[2].
KU-177 (10 μM; 24 h) exhibits the ability to disrupt interactions between Aha1 and Hsp90 in SH-SY5Y neuroblastoma cells and SK-BR-3 breast cancer cells, without significantly inhibition on Hsp90 client protein (Her2)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:ARP1 and H929 WT and AHSA1-OE cells
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Concentration:1 nM-100 μM
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Incubation Time:24, 48, 72 hours
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Result:Decreased multiple myeloma (MM) cell proliferation and PI resistance induced by AHSA1/HSP90 in vitro.
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Cell Line:SH-SY5Y neuroblastoma cells and Her2 overexpressing SK-BR-3 breast cancer cells
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Concentration:10 μM
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Incubation Time:24 hours
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Result:Didn’t induce the degradation of Hsp90 client proteins Her2 (in SK-BR-3 cells), Cdk6, or pAktS473 (in SHSY5Y cells), nor induced the expression of Hsp70, a marker of the heat shock response.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5TMM3VT mouse model (6-8 weeks old, C57BL/KaLwrij mice)[1]
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection; twice a week; sacrificed mice with hindlimb weakness immediately, about 4-5 weeks
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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.
Chemical Information
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CAS No. 1160952-43-1
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Appearance Solid
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Molecular Weight 489.47
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Formula C27H23NO8
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Color White to off-white
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SMILES
COC1=CC(C2=C(C=CC(C(NC3=CC4=CC=C(C(OC)=C4OC3=O)OC(C)=O)=O)=C2)OC)=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KU-177 Related Classifications
HY-151335 Related Classifications
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