RA-9

SKU: orb1298912

Description

RA-9 is a potent, selective inhibitor of proteasome-associated deubiquitinating enzymes (DUBs) with demonstrated anticancer activity. It selectively triggers apoptosis in ovarian cancer cell lines in vitro and has shown a favorable toxicity profile in preclinical research, supporting its investigation in oncology and ubiquitin-proteasome system studies.

Research Area

Cell Biology, Molecular Biology, Protein Biochemistry

Key Properties

• CAS Number: 919091-63-7
• MW: 365.34
• Purity: 98.15% (May vary between batches)
• Formula: C₁₉H₁₅N₃O₅
• SMILES: [O-][N+](=O)c1ccc(\C=C2/CNC\C(=C/c3ccc(cc3)[N+]([O-])=O)C2=O)cc1
• Target: Apoptosis|||DUB
• Solubility: DMSO:4 mg/mL (10.95 mM)

Bioactivity

• In Vivo:
  In vivo treatment with RA-9 retards tumor growth, increases overall survival, and was well tolerated by the host.
• In Vitro:
  The characterization of RA-9 as a small-molecule inhibitor of proteasome-associated DUBs. Treatment with RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. Loss of cell viability following RA-9 exposure is associated with an unfolded protein response as mechanism to compensate for unsustainable levels of proteotoxic stress.
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• Animal Research:
  Mice were inoculated i.p. with 100,000 ES-2 cells (in 100 μl DMEM) stably expressing GFP. When tumor was detectable (approx. 6 days post inoculation), mice were randomly assigned into two groups receiving RA-9 or 0.9% saline. Treatment with RA-9 was given i.p. on a one-day on, two-days off schedule. The control group received the vehicle alone at the same schedule. Working concentrations of RA-9 (10 mg/ml) were reached by dissolution in Cremophor EL and polyethylene glycol 400 (Sigma). Prior to each injection RA-9 was further diluted in 0.9% saline (working concentration 1mg/ml). To monitor for tumor growth, RA-9 treated and control mice were imaged with an IVIS SpectrumCT Pre-clinical in vivo imaging system (PerkinElmer) every other day. Animals were sacrificed when abdomens became distended to twice normal size.
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Storage & Handling

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

Alternative Names

cells, deubiquitinating enzymes (DUBs), Deubiquitinase, DUBs, Apoptosis, cancer, Inhibitor, inhibit, ovarian, Protein, RA9, RA-9, RA 9, survival, Response, Unfolded

Compound Identifiers

PubChem CID

5469266