For research use only. Not for therapeutic Use.
PRGL493 is a potent and selective long-chain acyl-CoA synthetase 4 (ACSL4) inhibitor. PRGL493 blocks cell proliferation and tumor growth in both breast and prostate cellular and animal models. PRGL493 is used for cancer research[1].
Acyl-CoA synthetase 4 (ACSL4) is an isoenzyme of the fatty acid ligase-coenzyme-A family taking part in arachidonic acid metabolism and steroidogenesis[1].PRGL493 ([3H]-AA (0.5 μCi/ml in serumfree medium) for 3 h; 48 hours) signifcantly inhibits the activity of ACSL4 in all three cell lines (MDA-MB-231, PC-3 and MA-10 Leydig cells), as evidenced by a reduction in AA-CoA levels.But PRGL493 has no effects on ACSL4 protein expression[1].
PRGL493 (20-100 μM; 72 hours) inhibits the proliferation of highly aggressive breast and prostate cancer cells at an IC50 of 23 μM and 27 μM, respectively[1].
PRGL493 (intraperitoneal injection; 250 μg/Kg; 43 and 34 consecutive days) decreases tumor volumes and inhibits tumor growth. Additionally, this compound results in a decrease in Ki67 protein expression and increases ER and AR expression in breast and prostate xenograft tumors, respectively[1].
| Catalog Number | I035011 |
| CAS Number | 2479378-45-3 |
| Synonyms | N-[4-[3-(5-methylfuran-2-yl)-1-phenylpyrazol-4-yl]-1,4-dihydro-[1,3,5]triazino[1,2-a]benzimidazol-2-yl]acetamide |
| Molecular Formula | C25H21N7O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H21N7O2/c1-15-12-13-21(34-15)22-18(14-31(30-22)17-8-4-3-5-9-17)23-28-24(26-16(2)33)29-25-27-19-10-6-7-11-20(19)32(23)25/h3-14,23H,1-2H3,(H2,26,27,28,29,33) |
| InChIKey | QNWGOBIYAPLFMK-UHFFFAOYSA-N |
| SMILES | CC1=CC=C(O1)C2=NN(C=C2C3N=C(NC4=NC5=CC=CC=C5N34)NC(=O)C)C6=CC=CC=C6 |
| Reference | [1]. Ana F Castillo, et al. New inhibitor targeting Acyl-CoA synthetase 4 reduces breast and prostate tumor growth, therapeutic resistance and steroidogenesis. Cell Mol Life Sci. 2021 Mar;78(6):2893-2910. |
