Cephaeline

SKU: orb1297429

Description

Cephaeline

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Immunology & Inflammation, Infectious Disease & Virology, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 483-17-0
• MW: 466.61
• Purity: 99.94% (May vary between batches)
• Formula: C₂₈H₃₈N₂O₄
• SMILES: [H][C@@]12C[C@H](C[C@H]3NCCc4cc(O)c(OC)cc34)[C@@H](CC)CN1CCc1cc(OC)c(OC)cc21
• Target: Influenza Virus,Virus Protease,ROS,Reactive Oxygen Species,Anti-infection,HIF,Nrf2,Ferroptosis
• Solubility: Ethanol:33.33 mg/mL (71.43 mM);DMSO:100 mg/mL (214.31 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.57 mM)

Bioactivity

• In Vitro:
  We compared the transcriptomes of primary CLL cells cocultured or not with protective bone marrow stromal cells (BMSCs) and found that oxidative phosphorylation, mitochondrial function, and hypoxic signaling undergo most significant dysregulation in non-protected CLL cells, with the changes peaking at 6-8 h, directly before induction of apoptosis. A subset of CLL patients displayed a gene expression signature resembling that of cocultured CLL cells and had significantly worse progression-free and overall survival. To identify drugs blocking BMSC-mediated support, we compared the relevant transcriptomic changes to the Connectivity Map database. Correlation was found with the transcriptomic signatures of the cardiac glycoside ouabain and of the ipecac alkaloids emetine and Cephaeline. These compounds were highly active against protected primary CLL cells (relative IC50's 287, 190, and 35 nM, respectively) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis. We tested emetine in a murine model of CLL and observed decreased CLL cells in peripheral blood, spleen, and bone marrow, recovery of hematological parameters and doubling of median survival (31.5 vs. 15 days, P = 0.0001).
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Storage & Handling

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

Alternative Names

Zika, phenolic, Virus Protease, VirusProtease, virus, NSC32944, NSC-32944, Inhibitor, NSC 32944, inhibit, Influenza Virus, InfluenzaVirus, Filovirus, HIF-1α, HIF-1, alkaloid, Cephaeline, Ebola

Compound Identifiers

PubChem CID

442195