| Name | Cephaeline |
| Description | Cephaeline was highly active against protected primary CLL cells (relative IC50's 35nM ) and acted by repressing HIF-1α± and disturbing intracellular redox homeostasis. |
| 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). |
| Storage | 02 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 33.33 mg/mL (71.43 mM), Sonication is recommended.
DMSO : 100 mg/mL (214.31 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (8.57 mM), Sonication is recommended.
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| Keywords | Zika | VirusProtease | Virus Protease | virus | phenolic | NSC-32944 | NSC32944 | NSC 32944 | Inhibitor | inhibit | InfluenzaVirus | Influenza Virus | HIF-1α | HIF-1 | Filovirus | Ebola | Cephaeline | alkaloid |
| Inhibitors Related | Ethoxyquin | Kaolin | Aceglutamide | Allopurinol | Hemin | Cysteamine hydrochloride | Ethyl linoleate | Magnesium acetate tetrahydrate | (E)-3-(p-Tolyl)acrylaldehyde | Thymidine | Dimethyl phthalate | Sodium Molybdate |
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United States
