货号：K6382

储存条件：-20℃可保存3年。

产品描述

ERR (Estrogen Related Receptor) is a group of nuclear receptors that is closely related to the estrogen receptor. The main isoforms of ERR are ERRα, ERRβ and ERRγ. ERRs act as a site-specific transcription regulator and have been also shown to interact with estrogen and the transcription factor TFIIB by direct protein-protein contact. The binding and regulatory activities of ERRs have been demonstrated in the regulation of a variety of genes. Kaempferol is an inverse agonist of ERRα and ERRγ. Kaempferol dose-dependently inhibited ERRα and ERRγ activity at the concentrations of 5, 10, and 20 μM. Human cholangiocarcinoma (CCA) cells HCCC9810 or QBC939 were exposed to 30, 60, 90, 120 or 150 μM kaempferol. Kaempferol significantly inhibited the viability of CCA cells in a time and dose dependent way. Treatment to HepG2 cells by 10 μM kaempferol for 24h suppressed ERRα and ERRγ target genes PDK2 and PDK4. In a CCA QBC939 xenograft model established in nude mice, kaempferol was i.p. administrated daily at the dose of 20 mg/kg for 3 weeks. Kaempferol significantly inhibited tumor growth and the number of Ki-67 positive tumor cells was lower in kaempferol-treated group than that in the control group. In a BSA-challenged BALB/c mice model of asthma, oral administration of ≤20 mg/kg kaempferol blocked epithelial cell excrescence and smooth muscle hypertrophy.

作用机制

Kaempferol directly binds the ligand binding domains (LBD) of ERRs.

产品信息