1. Cell Cycle/DNA Damage
    Metabolic Enzyme/Protease
  2. HSP
  3. KU-177

KU-177 

Cat. No.: HY-151335
Handling Instructions

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.

KU-177 Chemical Structure

KU-177 Chemical Structure

CAS No. : 1160952-43-1

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Description

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].

IC50 & Target

HSP90

 

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 ℃) 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: ARP1 and H929 WT and AHSA1-OE cells
Concentration: 1 nM-100 μM
Incubation Time: 24, 48, 72 hours
Result: Decreased multiple myeloma (MM) cell proliferation and PI resistance induced by AHSA1/HSP90 in vitro.

Cell Proliferation Assay[2]

Cell Line: SH-SY5Y neuroblastoma cells and Her2 overexpressing SK-BR-3 breast cancer cells
Concentration: 10 μM
Incubation Time: 24 hours
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

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 (HY-10227) (1 mg/kg; i.p.)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

489.47

Formula

C27H23NO8

CAS No.
SMILES

COC1=CC(C2=C(C=CC(C(NC3=CC4=CC=C(C(OC)=C4OC3=O)OC(C)=O)=O)=C2)OC)=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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KU-177
Cat. No.:
HY-151335
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