| Bioactivity | 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]. |
| Target | IC50: ACSL4 |
| Invitro | 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]. |
| In Vivo | 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]. Animal Model: |
| Name | PRGL493 |
| CAS | 2479378-45-3 |
| Formula | C25H21N7O2 |
| Molar Mass | 451.48 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 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. |