| Bioactivity | PR280 is a potent inhibitor of dihydroceramide desaturase 1 (Des1) (IC50=700 nM). PR280 forms hydrogen bonds with the amino acid residues of Des1, and its cyclopropenone group may form a coordination with the iron center, thus stabilizing the binding to the active site of Des1 and inhibiting the sphingosine lipid synthesis pathway of dihydroceramide (dhCer) to form ceramide. PR280 can be used in the study of diseases related to sphingosine lipid metabolism, such as cancer and metabolic diseases[1]. |
| Formula | C27H49NO4 |
| Molar Mass | 451.68 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Rivero P, et al. Targeting dihydroceramide desaturase 1 (Des1): Syntheses of ceramide analogues with a rigid scaffold, inhibitory assays, and AlphaFold2-assisted structural insights reveal cyclopropenone PR280 as a potent inhibitor[J]. Bioorganic Chemistry, 2024: 107233. |