货号:A272671
同义名:
山柰酚
/ Kempferol; Robigenin
Kaempferol acts as an inverse agonist that directly binds ERRα and ERRγ. It is a natural flavonol with antitumor activity.
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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[3]. 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[4]. 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[5]. Treatment to HepG2 cells by 10 μM kaempferol for 24h suppressed ERRα and ERRγ target genes PDK2 and PDK4[4]. 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[5]. 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[6]. |
作用机制 | Kaempferol directly binds the ligand binding domains (LBD) of ERRs. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
B16-4A5 cells | Function assay | Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs, IC50=20 μM | 19615910 | ||
HEK293 FS cells | Function assay | Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=1.2 μM | 20731357 | ||
human A549 cells | 5-40 μM | Cytotoxicity assay | 72 h | Cytotoxicity against human A549 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay | 22871217 |
human BxPC3 cells | 5-40 μM | Cytotoxicity assay | 72 h | Cytotoxicity against human BxPC3 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay | 22871217 |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.49mL 0.70mL 0.35mL |
17.47mL 3.49mL 1.75mL |
34.94mL 6.99mL 3.49mL |
CAS号 | 520-18-3 |
分子式 | C15H10O6 |
分子量 | 286.24 |
SMILES Code | O=C(C1=C(O)C=C(O)C=C1O2)C(O)=C2C3=CC=C(O)C=C3 |
MDL No. | MFCD00016938 |
别名 | 山柰酚 ;Kempferol; Robigenin; Pelargidenolon; Indigo Yellow; Campherol; 3,4',5,7-Tetrahydroxyflavone; Trifolitin; Swartziol; Rhamnolutein; Pelargidenon; NSC 656277; Nimbecetin; NSC 407289 |
运输 | 蓝冰 |
InChI Key | IYRMWMYZSQPJKC-UHFFFAOYSA-N |
Pubchem ID | 5280863 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, room temperature |