fasn-in-3

FASN-IN-3 是脂肪酸合酶抑制剂。

Fasnall, a fatty acid synthase (FASN) inhibitor, exhibits an IC50 of 3.71 μM against the human recombinant enzyme. It halts tritiated acetate incorporation into lipids (IC50= 5.84 μM), boosts ceramide levels, and triggers lipid droplet formation in BT474 HER2+ breast cancer cells. Demonstrating antiproliferative effects on various breast cancer cell lines, including non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3, its efficacy is directly linked to FASN expression in vitro. In murine models of HER2+ breast cancer, particularly the MMTV-Neu model, Fasnall significantly reduces tumor volume and extends survival. Furthermore, it enhances the efficacy of carboplatin in vivo, bolstering the objective response rate of stable disease from 25% with carboplatin alone to 88% when paired with Fasnall.

Octyl Orlistat, 作为一种潜在的脂肪酸合成酶(FASN)抑制剂, 在减少肿瘤细胞增殖方面显示出显著成效。通过靶向FASN并引发细胞凋亡，Orlistat 正被研究用作抗肿瘤化合物。与Cerulenin和C75相比，Orlistat在细胞培养和细胞系中表现出更高的抑制效力。在LN229细胞中，使用200 µM Orlistat处理48小时后，细胞生长减少了63.9 ± 8.7%，而在LT68细胞中细胞生长的减少率为76.3 ± 23.7%。经Orlistat处理的器官型切片培养显示，在Ki67染色后增殖减少，并观察到caspase-3的增加剪切。

CTL-06是一种Fatty Acid Synthase (FASN)抑制剂，具有3 μM的IC50，能够诱发细胞凋亡。CTL-12导致细胞周期在Sub-G1 S期停滞，并增加caspase-9和凋亡标志物Bax的表达，减少抗凋亡标志物Bcl-xL的表达。此外，CTL-12通过抑制脂肪酸的从头合成，剥夺肿瘤细胞代谢所需，主要用于乳腺癌和结直肠癌的研究。