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CAS No.: 520-18-3

山奈酚 Catalog No. CSN16382

Synonyms: 山奈酚;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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靶点选择性

生物活性

实验方案

技术信息

生物活性

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.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02425436	Intrauterine Growth Restrictio... more >>n (IUGR) Collapse <<	Phase 2	Completed	-	-
NCT02760017	Diabetes	Not Applicable	Completed	-	Brazil ... more >> Universidade do Extremo Sul Catarinense Criciuma, Santa Catarina, Brazil, 88801450 Collapse <<
NCT02191241	Healthy	Phase 1	Completed	-	-

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4936 mL
- 17.4681 mL
- 34.9362 mL
- 5 mM
- 0.6987 mL
- 3.4936 mL
- 6.9872 mL
- 10 mM
- 0.3494 mL
- 1.7468 mL
- 3.4936 mL

技术信息

CAS号

520-18-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H10O6

运输

蓝冰

分子量

286.24

别名

山奈酚;Kempferol;Robigenin

溶解度

DMSO	26.0 mg/mL (90.8 mM) warming
Water	Insoluble
Ethanol	27.0 mg/mL (94.3 mM)

动物实验配方

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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
human HeLa cells	-	Function assay	-	Inhibition of MRP1 transfected in human HeLa cells assessed as inhibition of [3H]LTC4 transport by rapid filtration assay, Ki=2.4 μM	19725578
human HL60 cells	-	Cytotoxicity assay	-	Cytotoxicity against human HL60 cells assessed as cell survival at 50 uM after 72 hrs by CCK8 assay	25074815
human MCF7 cells	5-40 μM	Cytotoxicity assay	72 h	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay	22871217
human MDA-kb2 cells	-	Function assay	-	Antagonist activity at androgen receptor in human MDA-kb2 cells assessed as inhibition of DHT-induced luciferase activity by luciferase reporter gene assay, IC50=9.7 μM	19592245
human MV4-11 cells	-	Cytotoxicity assay	72 h	Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=3.34 μM	23411073
human NCI-H2126 cells	5-40 μM	Cytotoxicity assay	72 h	Cytotoxicity against human NCI-H2126 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay	22871217
human PANC1 cells	5-40 μM	Cytotoxicity assay	72 h	Cytotoxicity against human PANC1 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay	22871217
human SMMC7721 cells	5-40 μM	Cytotoxicity assay	72 h	Cytotoxicity against human SMMC7721 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay	22871217
human U87 cells	5-40 μM	Cytotoxicity assay	72 h	Cytotoxicity against human U87 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay	22871217
MDA-MB-231 cells	5-40 μM	Cytotoxicity assay	72 h	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay	22871217
MDCK cells	-	Function assay	-	Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=4.7 μM	21354800
MDCK cells	50 μM	Function assay	-	Antiviral activity against influenza A virus H1N1 A/PR/8/34 infected in MDCK cells assessed as reduction in fluorescence positive cells at 50 uM immunofluorescence assay	19729316
mouse 3T3L1 cells	-	Function assay	-	Inhibition of AMPK-mediated adipocyte differentiation in mouse 3T3L1 cells	20822902
mouse L929 cells	-	Function assay	-	Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality treated with drug after 2 hrs of TNFalpha treatment	9287415
mouse RAW264.7 cells	-	Function assay	-	Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as nitrite level at 1 to 100 uM after 24 hrs by Griess method	21353543

山奈酚 Catalog No. CSN16382

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