KU-177

SKU: orb1686769

Description

KU-177 is a small molecule inhibitor targeting the Hsp90 co-chaperone Aha1. By disrupting the Hsp90-Aha1 interaction, it inhibits proliferation and overcomes proteasome inhibitor resistance in multiple myeloma (MM) cell lines and primary patient samples, supporting its investigation as a potential therapeutic agent.

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 1160952-43-1
• MW: 489.47
• Purity: 98.54% (May vary between batches)
• Formula: C₂₇H₂₃NO₈
• SMILES: O=C1OC=2C(OC)=C(OC(=O)C)C=CC2C=C1NC(=O)C3=CC=C(OC)C(=C3)C4=CC=CC(OC)=C4
• Target: HSP

Bioactivity

• Target IC50:
  Aha1/HSP90:4.08 μM
• In Vivo:
  In the 5TMM3VT multiple myeloma mouse model, KU-177 (1 mg/kg, intraperitoneal injection twice weekly for 4 weeks) was able to inhibit tumor growth and prolong survival without showing significant toxicity. When combined with Bortezomib (1 mg/kg, intraperitoneal injection), KU-177 demonstrated more significant therapeutic effects in vivo.
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• In Vitro:
  KU-177 (50 μM, 48 hours of action) was able to inhibit the proliferation of flow MRD-positive cells in samples from patients with primary and relapsed multiple myeloma (MM). In AHSA1 WT/OE cells, PSMD2 WT/OE cells and ANBL6 WT/DR cells, KU-177 (30 μM, treated for 48 hours) decreased proteasome activity. KU-177 disrupts the interaction of Aha1 with Hsp90 with an IC50 value of 4.08 μM without affecting the ATPase activity of Hsp90. KU-177 (25 μM, incubated at 37°C for 30 min) inhibits the aggregation of recombinant P301L tau protein but does not affect the refolding of fluorokinase by inhibiting Hsp90. KU-177 (10 μM, treated for 24 hours) exhibits the ability to disrupt the interaction of Aha1 with Hsp90 in SH-SY5Y neuroblastoma cells and SK-BR-3 breast cancer cells, while not significantly inhibiting the Hsp90 client protein Her2.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KU177

Compound Identifiers

PubChem CID

53261526