Praelolide

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Praelolide

CAS No. :

MCE 国际站：Praelolide

产品活性：Praelolide 是一种有效的 Nrf2 激活剂。Praelolide 抑制破骨细胞生成和活性氧 (ROS) 的产生。Praelolide 通过与 Keap1 的非共价结合来破坏 Keap1-Nrf2 蛋白质-蛋白质相互作用。Praelolide 具有用于破骨细胞性骨病研究的潜力。

研究领域：NF-κB

作用靶点：Keap1-Nrf2  |  NF-κB

In Vitro: Praelolide (compound 21) (10 µM) shows anti-osteoclastogenesis activities with the inhibitory ratio of 100% in bone marrow monocytes/macrophages (BMMs).
Praelolide (1, 1.25, 5, 10 µM; 1-5 days) inhibits RANKL-induced osteoclast formation with no cytotoxicity, and inhibits bone resorption of osteoclasts and actin ring formation in BMMs.
Praelolide (5, 10 µM) inhibits RANKL-induced mRNA levels of NFATc1, cathepsin K, MMP-9 and TRAP in BMMs.
Praelolide (5, 10 µM; 6 h) increases the protein expression of Nrf2, HO-1 and NQO1, enhances the stability of Nrf2 protein.
Praelolide (10 µM; 0-60 min) inhibits RANKL-induced NF-κB and MAPK signaling pathways and inhibits RANKL-induced phosphorylation of ERK, p38 MAPK, IKBα, and p65 NF-kB in pre-osteoclasts.
Praelolide (0, 20, 50, 100 µM; 24 h) interferes the interaction between Keap1 and Nrf2 by binding to Keap1 protein in RAW264.7 cells.

In Vivo: Praelolide (2, 5, 10 µM; co-treated for 6 days) rescues the bone loss of prednisone-induced zebrafish.

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