Page last updated: 2024-11-11

icaritin

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Description

icaritin: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5318980
CHEMBL ID498485
SCHEMBL ID4223542
MeSH IDM0483270

Synonyms (42)

Synonym
BIDD:ER0021
118525-40-9
4h-1-benzopyran-4-one, 3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-buten-1-yl)-
3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-buten-1-yl)-4h-1-benzopyran-4-one
bdbm50272527
3-hydroxy-7-o-beta-glucose-8-prenyl-4''-methoxy chrysin
sgn162
CHEMBL498485 ,
sgn-162
icaritin
3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-enyl)chromen-4-one
unii-ufe666uely
ufe666uely ,
S9080
FT-0670266
NCGC00345813-01
4h-1-benzopyran-4-one, 3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-butenyl)-
AKOS015896858
icaritin [who-dd]
TUUXBSASAQJECY-UHFFFAOYSA-N
MLS006010055
smr004701218
CS-3679
SCHEMBL4223542
AC-33950
HY-N0678
I0974
DTXSID00152154
icartin
icaritin, >=98% (hplc)
icaritin(anhydroicaritin)
DB12672
3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-4h-chromen-4-one
mfcd22422519
cycloicaritin
BCP32968
NCGC00345813-04
CCG-268265
Q27291061
AS-55987
4'-methoxy-3,5,7trihydroxy-8-3,3-dimethylallylflavone
3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-enyl)-4h-chromen-4-one

Research Excerpts

Overview

Icaritin is a prenylflavonoid present in the Chinese herbal medicinal plant Epimedium spp. It is a promising anti-hepatoma drug that is currently being tested in a phase-III clinical trial.

ExcerptReferenceRelevance
"Icaritin is an active ingredient in "( Design, Synthesis, and Biological Evaluation of Icaritin Derivatives as Novel Putative DEPTOR Inhibitors for Multiple Myeloma Treatment.
Cheng, H; Hou, Y; Kuang, W; Liu, Z; Min, W; Pu, S; Sun, C; Wang, L; Wang, X; Xiao, Y; Xin, GZ; Yang, P; Yuan, K; Zhang, F, 2021
)
2.32
"Icaritin (ICT) is a metabolite of icariin (ICA), which are two active flavonoid components extracted from"( Therapeutic Effect of Icaritin on Cerebral Ischemia-Reperfusion-Induced Senescence and Apoptosis in an Acute Ischemic Stroke Mouse Model.
Chen, CM; Chen, MC; Guan, SS; Liu, SH; Wu, CT; Yang, TH, 2022
)
1.76
"Icaritin is a prenylflavonoid present in the Chinese herbal medicinal plant Epimedium spp. "( Complete biosynthesis of the potential medicine icaritin by engineered Saccharomyces cerevisiae and Escherichia coli.
Huang, W; Li, C; Li, X; Wang, J; Wang, P; Wang, Y; Yan, X; Yang, X; Zhang, Y; Zhou, Z, 2021
)
2.32
"Icaritin is an aglycone of flavonoid glycosides from Herba Epimedii. "( Highly efficient bioconversion of icariin to icaritin by whole-cell catalysis.
Chen, WW; Ding, B; Du, LQ; Guo, M; Huang, RB; Liang, M; Lin, Y; Pang, H; Wei, YT, 2023
)
2.61
"Icaritin (ICT) is a natural compound extracted from anti-osteoporosis herb"( Icaritin ameliorates RANKL-mediated osteoclastogenesis and ovariectomy-induced osteoporosis.
Chen, K; Huang, JM; Jiang, AL; Lai, Q; Qi, GB; Wang, XH; Wang, Z; Zhang, YQ, 2023
)
3.07
"Icaritin (ICT) is a traditional Chinese herbal medicine that exhibits antitumor efficacy in variety of cancers including PCa."( Anticancer effect of icaritin on prostate cancer via regulating miR-381-3p and its target gene UBE2C.
Ding, Q; Hu, J; Hu, M; Jiang, H; Ma, C; Rashid, K; Wu, X; Yang, C, 2019
)
1.55
"Icaritin is a promising anti-hepatoma drug that is currently being tested in a phase-III clinical trial. "( Preparation, Characterization, and In Vivo Evaluation of Amorphous Icaritin Nanoparticles Prepared by a Reactive Precipitation Technique.
Chen, X; Jin, M; Kong, J; Li, F; Liang, H; Meng, K; Tang, C; Yao, H; Yin, H; Yuan, Q, 2021
)
2.3
"1. Icaritin is a natural flavonoid with anti-osteoporosis activity. "( Glucuronidation of icaritin by human liver microsomes, human intestine microsomes and expressed UDP-glucuronosyltransferase enzymes: identification of UGT1A3, 1A9 and 2B7 as the main contributing enzymes.
Dai, Y; Gonzalez, FJ; Hong, X; Qin, Z; Wang, L; Wu, B; Yao, X; Yao, Z; Zhao, G, 2018
)
1.43
"Icaritin is a compound extracted from herb, recent study have found it is able to influence the activity of various types of cancer. "( Effects of Icaritin on the physiological activities of esophageal cancer stem cells.
Chen, M; Dong, X; Gou, Y; Han, S; Jin, D; Ma, J, 2018
)
2.31
"Icaritin (ICT) is a hydrolytic form of icariin isolated from plants of the genus Epimedium. "( Icaritin synergistically enhances the radiosensitivity of 4T1 breast cancer cells.
Chen, C; Han, D; Hong, J; Li, S; Lv, W; Yang, S; Zhang, L; Zhang, M; Zhang, W; Zhang, Z, 2013
)
3.28
"Icaritin (ICT) is a hydrolytic product of Icariin."( Icaritin attenuates cigarette smoke-mediated oxidative stress in human lung epithelial cells via activation of PI3K-AKT and Nrf2 signaling.
Dong, J; Wong, PF; Wu, J; Xia, S; Xu, H; Xu, J, 2014
)
2.57
"Icaritin (ICT) is a major bioactive prenylflavonoid derivative contained in the Epimedium which is a widely used herbal medicine for the treatment of infertility, impotence, cardiovascular and skeletal diseases listed in the Chinese Pharmacopoeia. "( Biodistribution evaluation of icaritin in rats by ultra-performance liquid chromatography-tandem mass spectrometry.
Zhang, SQ, 2014
)
2.13
"Icaritin is an active ingredient derived from the plant Herba epimedium, which exhibits various pharmacological and biological activities. "( Anticancer agent icaritin induces apoptosis through caspase-dependent pathways in human hepatocellular carcinoma cells.
Gong, L; Peng, Q; Qu, L; Si, J; Sun, L, 2015
)
2.2
"Icaritin is an active prenylflavonoid derived from Epimedium genus, a traditional Chinese medicine. "( Icaritin suppresses multiple myeloma, by inhibiting IL-6/JAK2/STAT3.
Dai, C; Deng, M; Li, R; Li, Z; Liu, S; Luo, Y; Peng, H; Wang, Z; Xu, Y; Zhang, G; Zhu, S, 2015
)
3.3
"Icaritin (ICT) is a traditional Chinese medicinal herb proved to be neuroprotective and exerts promoting effects on cardiac differentiation. "( Icaritin Attenuates Myocardial Ischemia and Reperfusion Injury Via Anti-Inflammatory and Anti-Oxidative Stress Effects in Rats.
Shi, J; Xing, B; Yang, L; Zhang, W; Zhou, X, 2015
)
3.3
"Icaritin (ICT) is an active monomer extracted from Chinese herbals named the Epimedium genus."( The role of icaritin in regulating Foxp3/IL17a balance in systemic lupus erythematosus and its effects on the treatment of MRL/lpr mice.
Chan, TM; Dai, Y; Li, D; Liao, J; Liu, Y; Long, H; Lu, Q; Tan, Y; Wu, H; Yung, S; Zhao, M, 2016
)
1.53
"Icaritin (IT) is a flavonoid isolated from Herba Epimedii. "( Iciartin, a novel FASN inhibitor, exerts anti-melanoma activities through IGF-1R/STAT3 signaling.
Cao, H; Du, J; Fu, X; Li, T; Liu, B; Su, T; Tse, AK; Wu, J; Xu, J; Yu, ZL, 2016
)
1.88
"Icaritin (ICT) is a prenyl flavonoid derived from the Epimedium genus, which has many biological and pharmacological effects."( Antitumoral action of icaritin in LNCaP prostate cancer cells by regulating PEA3/HER2/AR signaling.
Hu, J; Hu, M; Jiang, H; Mao, S; Wei, B; Wen, H; Xu, H; Yang, T; Zhu, W, 2016
)
1.47
"Icaritin is an active ingredient extracted from the plant Herba Epimedium Sagittatum (Sieb. "( Icaritin induces cell death in activated hepatic stellate cells through mitochondrial activated apoptosis and ameliorates the development of liver fibrosis in rats.
Cao, L; Li, J; Liao, J; Liu, P; Qian, H; Wu, M; Xu, W; Yin, Z; Zhang, R, 2011
)
3.25
"Icaritin is a native compound from Epimedium Genus, a traditional Chinese herbal medicine which is effective in treating asthma, autoimmune diseases and viral infections. "( Icaritin inhibits T cell activation and prolongs skin allograft survival in mice.
He, L; Hu, Y; Li, X; Liu, S; Wang, S; Zhou, H, 2012
)
3.26
"Icaritin (ICT) is a main aglycone and also active intestinal metabolite of prenylflavonoids from the Chinese medicine Herba Epimedii. "( Oral absorption and excretion of icaritin, an aglycone and also active metabolite of prenylflavonoids from the Chinese medicine Herba Epimedii in rats.
Chang, Q; Li, Y; Wang, GN; You, C; Zhang, L; Zheng, Y, 2012
)
2.1

Effects

Icaritin has a wide range of pharmacological and biological activities, including cardiovascular function improvement, hormone regulation and antitumor activity.

Icaritin (ICT) has been previously demonstrated to display protective effects against cerebral ischemic reperfusion (I/R) by inhibiting oxidative stress. Icaritin has a wide range of pharmacological activities, including significant an-titumor activity.

ExcerptReferenceRelevance
"Icaritin has a wide range of pharmacological activities, including significant an-titumor activity. "( Icaritin inhibits endometrial carcinoma cells by suppressing O-GlcNAcylation of FOXC1.
Kong, Y; Liu, Y; Wang, G; Wang, Y; Yang, F; Zhang, H, 2023
)
3.8
"Icaritin has a wide range of pharmacological and biological activities, including cardiovascular function improvement, hormone regulation and antitumor activity."( Icaritin suppresses multiple myeloma, by inhibiting IL-6/JAK2/STAT3.
Dai, C; Deng, M; Li, R; Li, Z; Liu, S; Luo, Y; Peng, H; Wang, Z; Xu, Y; Zhang, G; Zhu, S, 2015
)
2.58
"Icaritin has potential anticancer effects on various cancers, including multiple myeloma (MM). "( Icaritin-elevated circ_0000190 suppresses the malignant progression of multiple myeloma by targeting miR-301a.
Chai, J; Zhang, Q; Zhang, XR; Zhu, YH, 2022
)
3.61
"Icaritin (ICT) has been previously demonstrated to display protective effects against cerebral ischemic reperfusion (I/R) by inhibiting oxidative stress, but the mechanism remains unclear. "( UHPLC-ESI-QE-Orbitrap-MS based metabolomics reveals the antioxidant mechanism of icaritin on mice with cerebral ischemic reperfusion.
Feng, Z; Liu, Z; Sun, C; Sun, L; Tang, Y; Yao, J; Zhang, G; Zhao, Y, 2023
)
2.58
"Icaritin has a wide range of pharmacological activities, including significant an-titumor activity. "( Icaritin inhibits endometrial carcinoma cells by suppressing O-GlcNAcylation of FOXC1.
Kong, Y; Liu, Y; Wang, G; Wang, Y; Yang, F; Zhang, H, 2023
)
3.8
"Icaritin has a wide range of pharmacological and biological activities, including cardiovascular function improvement, hormone regulation and antitumor activity."( Icaritin suppresses multiple myeloma, by inhibiting IL-6/JAK2/STAT3.
Dai, C; Deng, M; Li, R; Li, Z; Liu, S; Luo, Y; Peng, H; Wang, Z; Xu, Y; Zhang, G; Zhu, S, 2015
)
2.58
"Icaritin has selective estrogen receptor (ER) modulating activity. "( Icaritin induces growth inhibition and apoptosis of human prostatic smooth muscle cells in an estrogen receptor-independent manner.
Chen, MF; Dai, YQ; Li, Y; Qi, L; Zhang, P; Zu, XB, 2010
)
3.25

Actions

Icaritin (ICT) displays numerous pharmacological activities for the treatment of various cancers, osteoporosis, inflammation, and angiocardiopathy. Icaritin promotes platelet production and regulates T cell polarization, but its mechanism is not clear.

ExcerptReferenceRelevance
"Icaritin can enhance radiosensitivity of NPC cells both "( [Icaritin increases radiosensitivity of nasopharyngeal carcinoma cells by regulating iron death].
Gou, W; Hou, W; Hu, T; Li, Y; Liu, G; Ren, Z; Zuo, D, 2023
)
3.26
"Icaritin can inhibit cell proliferation and induce apoptosis in Oral Squamous Cell Carcinoma (OSCC). "( Stable Loading and Delivery of Icaritin Using PEG-PCL Micelles for Effective Treatment of Oral Squamous Cell Carcinoma.
Chen, XJ; Yang, JG; Zhang, J; Zhou, G, 2021
)
2.35
"Icaritin can inhibit cell proliferation and induce apoptosis of KM3/BTZ cells, moreover, can effectively reverse the multidrug resistance of KM3/BTZ cells. "( [Icaritin Reverses Multidrug Resistance of Multiple Myeloma Cell Line KM3/BTZ].
Chen, X; Fang, J; Fang, ZQ; Huang, XR; Li, ZJ; Li, ZY; Zhang, JG, 2017
)
2.81
"Icaritin promotes platelet production and regulates T cell polarization, but its mechanism is not clear."( Icaritin Provokes Serum Thrombopoietin and Downregulates Thrombopoietin/MPL of the Bone Marrow in a Mouse Model of Immune Thrombocytopenia.
Dai, Z; Liu, R; Liu, X; Pu, X; Sun, Y; Tian, F; Zhang, K; Zhao, X, 2018
)
2.64
"Icaritin can inhibit proliferation and induce apoptosis of THP-1 in vitro, Icaritin may induce apoptosis in THP-1 cells through the mitochondrial pathway."( [Effect of Icaritin on Proliferation and Apoptosis of THP-1 Cell and Its Mechanism].
Kuang, WY; Li, RJ; Zhang, GS; Zheng, MC, 2017
)
2.29
"Icaritin (ICT) displays numerous pharmacological activities for the treatment of various cancers, osteoporosis, inflammation, and angiocardiopathy. "( Oral absorption, distribution, metabolism, and excretion of icaritin in rats by Q-TOF and UHPLC-MS/MS.
Zhang, SQ; Zhang, SZ, 2017
)
2.14

Treatment

Icaritin treatment caused a rapid increase in ROS in HeLa and SiHa cells, which was followed by a prominent increase in the number of DNA strand breaks. Icaritin pretreatment significantly inhibited the elevation of intracellular Ca(2+) induced by LPS.

ExcerptReferenceRelevance
"Icaritin treatment caused a rapid increase in ROS in HeLa and SiHa cells, which was followed by a prominent increase in the number of DNA strand breaks."( Reactive oxygen species induced by icaritin promote DNA strand breaks and apoptosis in human cervical cancer cells.
Chen, X; Hou, Y; Li, F; Song, L, 2019
)
1.51
"Icaritin treatment induced immune biomarkers and immune-modulating activities in myeloid cells were also explored."( First-in-class immune-modulating small molecule Icaritin in advanced hepatocellular carcinoma: preliminary results of safety, durable survival and immune biomarkers.
Ding, X; Fan, Y; Hao, R; Jiang, J; Li, S; Li, Y; Liu, K; Meng, K; Qiu, W; Wang, S; Xu, B; Ye, B; Yue, J; Zhao, H; Zheng, L, 2019
)
1.49
"Icaritin treatment induced changes in immune biomarkers-and immune-suppressive myeloid cells were observed."( First-in-class immune-modulating small molecule Icaritin in advanced hepatocellular carcinoma: preliminary results of safety, durable survival and immune biomarkers.
Ding, X; Fan, Y; Hao, R; Jiang, J; Li, S; Li, Y; Liu, K; Meng, K; Qiu, W; Wang, S; Xu, B; Ye, B; Yue, J; Zhao, H; Zheng, L, 2019
)
1.49
"Icaritin pretreatment significantly inhibited the elevation of intracellular Ca(2+) induced by LPS."( Icaritin exhibits anti-inflammatory effects in the mouse peritoneal macrophages and peritonitis model.
Huang, X; Lai, X; Sun, C; Tang, X; Ye, Y; Yin, P; Zeng, X; Zeng, Y, 2013
)
2.55
"Icaritin treatment also induced expression of pro-apoptotic protein Bax with a concomitant decrease of Bcl-2 expression."( Icaritin causes sustained ERK1/2 activation and induces apoptosis in human endometrial cancer cells.
Fu, XQ; Hou, Y; Huang, X; Qi, ST; Sheng, J; Sun, QY; Tong, JS; Wang, YP; Zhang, QH, 2011
)
2.53
"Treatment of icaritin in both primary and established (HT-29) CRC cells induced feedback activation of autophagy, evidenced by p62 degradation, Beclin-1 and autophagy-related gene-5 (ATG-5) upregulation, as well as light chain 3B (LC3B)-GFP puncta formation."( AMPK-autophagy inhibition sensitizes icaritin-induced anti-colorectal cancer cell activity.
Chen, MB; Dong, D; Gu, J; Xu, D; Yang, Q; Zhang, G; Zhou, C, 2017
)
1.08
"When treated with icaritin for 24 to 72 h, cell growth was strongly inhibited (at 48 h IC(50) was 10.74+/-1.59 micromol/l, P<0.001) companied with a mitochondrial transmembrane potential (_Psim) drop."( A novel anticancer agent, icaritin, induced cell growth inhibition, G1 arrest and mitochondrial transmembrane potential drop in human prostate carcinoma PC-3 cells.
Huang, X; Lou, Y; Zhu, D, 2007
)
0.96

Toxicity

ExcerptReferenceRelevance
"No drug-related adverse events ≥ Grade 3 were observed in all 20 enrolled HCC patients."( First-in-class immune-modulating small molecule Icaritin in advanced hepatocellular carcinoma: preliminary results of safety, durable survival and immune biomarkers.
Ding, X; Fan, Y; Hao, R; Jiang, J; Li, S; Li, Y; Liu, K; Meng, K; Qiu, W; Wang, S; Xu, B; Ye, B; Yue, J; Zhao, H; Zheng, L, 2019
)
0.77

Pharmacokinetics

Icaritin can be used as a pharmacokinetic marker to reflect prenylflavonoid exposure levels, as well as the changes over time of its glucuronide conjugates.

ExcerptReferenceRelevance
"This study successfully elucidated the pharmacokinetic profiles of EWH extract and five EWH-derived prenylflavonoid monomers in rats."( Systematic considerations for a multicomponent pharmacokinetic study of Epimedii wushanensis herba: From method establishment to pharmacokinetic marker selection.
Jin, Y; Wang, C; Wu, C; Zhang, J, 2015
)
0.42
"The study was a comprehensive analysis of metabolic pathways and pharmacokinetic markers."( Systematic considerations for a multicomponent pharmacokinetic study of Epimedii wushanensis herba: From method establishment to pharmacokinetic marker selection.
Jin, Y; Wang, C; Wu, C; Zhang, J, 2015
)
0.42
" To select appropriate EWH-derived pharmacokinetic markers, a high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was established to simultaneously monitor 14 major compounds in unhydrolyzed plasma and 10 potential pharmacokinetic markers in hydrolyzed plasma."( Systematic considerations for a multicomponent pharmacokinetic study of Epimedii wushanensis herba: From method establishment to pharmacokinetic marker selection.
Jin, Y; Wang, C; Wu, C; Zhang, J, 2015
)
0.42
"The pharmacokinetic profiles indicated that the glucuronide conjugates of icaritin were the principle circulating metabolites and that total icaritin accounted for ∼99% of prenylflavonoid exposure after administration of EWH-derived materials to rats."( Systematic considerations for a multicomponent pharmacokinetic study of Epimedii wushanensis herba: From method establishment to pharmacokinetic marker selection.
Jin, Y; Wang, C; Wu, C; Zhang, J, 2015
)
0.65
"Icaritin in hydrolyzed plasma can be used as a pharmacokinetic marker to reflect prenylflavonoid exposure levels, as well as the changes over time of its glucuronide conjugates."( Systematic considerations for a multicomponent pharmacokinetic study of Epimedii wushanensis herba: From method establishment to pharmacokinetic marker selection.
Jin, Y; Wang, C; Wu, C; Zhang, J, 2015
)
1.86

Bioavailability

A novel combination of amorphization and nanonization was used to enhance the oral bioavailability of icaritin.

ExcerptReferenceRelevance
" In order to examine their bioavailability in humans, we have developed and validated a sensitive method to quantify icaritin and desmethylicaritin in human sera, using gas chromatography-mass spectrometry."( Sensitive and rapid method to quantify icaritin and desmethylicaritin in human serum using gas chromatography-mass spectrometry.
Shen, P; Wong, SP; Yong, EL, 2007
)
0.82
" The oral bioavailability of ICT was 35% of dose, estimated by its total plasma drug concentrations."( Oral absorption and excretion of icaritin, an aglycone and also active metabolite of prenylflavonoids from the Chinese medicine Herba Epimedii in rats.
Chang, Q; Li, Y; Wang, GN; You, C; Zhang, L; Zheng, Y, 2012
)
0.66
" However, its low bioavailability limits its clinical efficacy for the treatment of osteoporosis."( Mechanism of enhanced antiosteoporosis effect of circinal-icaritin by self-assembled nanomicelles in vivo with suet oil and sodium deoxycholate.
Feng, L; Jia, X; Jiang, J; Li, J; Sun, E; Zhang, Z, 2015
)
0.66
"In this paper, suet oil (SO) was used to improve the oral bioavailability of CIT and enhance its antiosteoporosis effect and absorption."( Mechanism of enhanced antiosteoporosis effect of circinal-icaritin by self-assembled nanomicelles in vivo with suet oil and sodium deoxycholate.
Feng, L; Jia, X; Jiang, J; Li, J; Sun, E; Zhang, Z, 2015
)
0.66
"The increased antiosteoporosis effects and bioavailability of CIT-SO-DOC self-assembled nanomicelles were due to an increase in absorption of CIT by reducing the particle sizes of CIT."( Mechanism of enhanced antiosteoporosis effect of circinal-icaritin by self-assembled nanomicelles in vivo with suet oil and sodium deoxycholate.
Feng, L; Jia, X; Jiang, J; Li, J; Sun, E; Zhang, Z, 2015
)
0.66
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" A novel combination of amorphization and nanonization was used to enhance the oral bioavailability of icaritin."( Preparation, Characterization, and In Vivo Evaluation of Amorphous Icaritin Nanoparticles Prepared by a Reactive Precipitation Technique.
Chen, X; Jin, M; Kong, J; Li, F; Liang, H; Meng, K; Tang, C; Yao, H; Yin, H; Yuan, Q, 2021
)
1.07
" IC-MEs significantly improve the bioavailability of IC due to the encapsulation of coix oil-based microemulsion and also obtain the desired liver accumulation and elimination."( An icaritin-loaded microemulsion based on coix oil for improved pharmacokinetics and enhanced antitumor efficacy.
Chen, Y; Li, X; Liu, Y; Qu, D; Zeng, H, 2022
)
1.34

Dosage Studied

ExcerptRelevanceReference
"Take conversion rate as index, the effects of pH, temperature, reaction time, dosage of enzyme, concentration of Icariin and metal ion on hydrolysis were studied by single-factor designs and a L9 (3(4)) orthogonal design."( [Study on preparation of icaritin by enzymolysis of icariin with snail hydrolase].
Chen, L; Jia, D; Jia, X; Shi, F; Sun, E; Xue, J; Zhang, Z, 2010
)
0.66
" However, one of the main disadvantages of the compound is the high volume and dosage during long-term administration period."( The beneficial effect of icaritin on osteoporotic bone is dependent on the treatment initiation timing in adult ovariectomized rats.
Bakker, AJ; Guo, B; He, Y; Hung, L; Leung, WN; Pan, X; Peng, S; Qin, L; Zhang, BT; Zhang, G; Zhen, W, 2013
)
0.69
" The relative bioavailabilities of CIT-SO high dosage, CIT-SO medium dosage, and CIT-SO low dosage (area under concentration-time curve [AUC]0-∞) compared with that of raw CIT high dosage, CIT medium dosage, and CIT low dosage (AUC0-∞) were 127%, 121%, and 134%, respectively."( Mechanism of enhanced antiosteoporosis effect of circinal-icaritin by self-assembled nanomicelles in vivo with suet oil and sodium deoxycholate.
Feng, L; Jia, X; Jiang, J; Li, J; Sun, E; Zhang, Z, 2015
)
0.66
" Meanwhile, mice in negative control group were treated with the same dosage of PBS."( [Icaritin prevents vascular calcification in mice].
Hua, Q; Ren, L; Tang, S; Wang, Z; Xie, H, 2019
)
1.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency22.53280.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Lysine-specific histone demethylase 1AHomo sapiens (human)IC50 (µMol)64.49000.00312.16029.6000AID1515260
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)2.20000.00001.18439.6140AID362785
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Processvia Protein(s)Taxonomy
regulation of double-strand break repair via homologous recombinationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of protein ubiquitinationLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of protein localizationLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to UVLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to gamma radiationLysine-specific histone demethylase 1AHomo sapiens (human)
DNA repair-dependent chromatin remodelingLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neuroblast proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
protein demethylationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of epithelial to mesenchymal transitionLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neuron projection developmentLysine-specific histone demethylase 1AHomo sapiens (human)
cerebral cortex developmentLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
neuron maturationLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA damage response, signal transduction by p53 class mediatorLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of cell sizeLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of DNA-templated transcriptionLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of transcription by RNA polymerase IILysine-specific histone demethylase 1AHomo sapiens (human)
guanine metabolic processLysine-specific histone demethylase 1AHomo sapiens (human)
muscle cell developmentLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of androgen receptor signaling pathwayLysine-specific histone demethylase 1AHomo sapiens (human)
response to fungicideLysine-specific histone demethylase 1AHomo sapiens (human)
cellular response to cAMPLysine-specific histone demethylase 1AHomo sapiens (human)
regulation of DNA methylation-dependent heterochromatin formationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of cold-induced thermogenesisLysine-specific histone demethylase 1AHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of neural precursor cell proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of stem cell proliferationLysine-specific histone demethylase 1AHomo sapiens (human)
chromatin remodelingLysine-specific histone demethylase 1AHomo sapiens (human)
positive regulation of cardiac muscle hypertrophycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of nitric oxide mediated signal transductioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cardiac muscle contractioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
relaxation of cardiac musclecGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
telomeric DNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
p53 bindingLysine-specific histone demethylase 1AHomo sapiens (human)
chromatin bindingLysine-specific histone demethylase 1AHomo sapiens (human)
transcription coactivator activityLysine-specific histone demethylase 1AHomo sapiens (human)
protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
oxidoreductase activityLysine-specific histone demethylase 1AHomo sapiens (human)
enzyme bindingLysine-specific histone demethylase 1AHomo sapiens (human)
nuclear receptor coactivator activityLysine-specific histone demethylase 1AHomo sapiens (human)
demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone H3K4 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
histone H3K9 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
identical protein bindingLysine-specific histone demethylase 1AHomo sapiens (human)
MRF bindingLysine-specific histone demethylase 1AHomo sapiens (human)
flavin adenine dinucleotide bindingLysine-specific histone demethylase 1AHomo sapiens (human)
nuclear androgen receptor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
telomeric repeat-containing RNA bindingLysine-specific histone demethylase 1AHomo sapiens (human)
DNA-binding transcription factor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
FAD-dependent H3K4me/H3K4me3 demethylase activityLysine-specific histone demethylase 1AHomo sapiens (human)
promoter-specific chromatin bindingLysine-specific histone demethylase 1AHomo sapiens (human)
transcription factor bindingLysine-specific histone demethylase 1AHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
chromatinLysine-specific histone demethylase 1AHomo sapiens (human)
nucleusLysine-specific histone demethylase 1AHomo sapiens (human)
chromosome, telomeric regionLysine-specific histone demethylase 1AHomo sapiens (human)
nucleusLysine-specific histone demethylase 1AHomo sapiens (human)
nucleoplasmLysine-specific histone demethylase 1AHomo sapiens (human)
transcription regulator complexLysine-specific histone demethylase 1AHomo sapiens (human)
protein-containing complexLysine-specific histone demethylase 1AHomo sapiens (human)
DNA repair complexLysine-specific histone demethylase 1AHomo sapiens (human)
cellular_componentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (78)

Assay IDTitleYearJournalArticle
AID1445698Antibacterial activity against Bacillus cereus ATCC 11778 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445704Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29737 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445710Antibacterial activity against methicillin-resistant Staphylococcus aureus BAA-38 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID362788Inhibition of human PDE6C at 10 uM2008Journal of natural products, Sep, Volume: 71, Issue:9
Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
AID1233700Cytotoxicity against human MCF7 cells assessed as cell viability by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Synthesis and cancer cell growth inhibitory activity of icaritin derivatives.
AID1445722Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-resistant Staphylococcus aureus ATCC BAA-382017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445733Membrane permeabilization activity in DOPE/DOPG large unilamellar liposomes assessed as leakage of calcein at 1:4 to 1:8 compound to lipid ratio by fluorescence assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445708Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1256913Inhibition of human IDH1 expressed in IPTG-induced Escherichia coli BL21 cells assessed as reduction of NADP+ to NADPH after 5 mins by spectrophotometry2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Discovery of α-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1.
AID1445706Antibacterial activity against methicillin-resistant Staphylococcus aureus DB68004 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID671762Inhibition of HCV NS3 helicase overexpressed in Escherichia coli BL21(DE3) assessed as inhibition of DNA unwinding activity at 10 uM by FRET assay2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification of myricetin and scutellarein as novel chemical inhibitors of the SARS coronavirus helicase, nsP13.
AID1445714Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-sensitive Staphylococcus aureus ATCC 292132017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1515260Inhibition of LSD1 (unknown origin) by fluorescence assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Flavone-based natural product agents as new lysine-specific demethylase 1 inhibitors exhibiting cytotoxicity against breast cancer cells in vitro.
AID1445696Antibacterial activity against Staphylococcus aureus DM4001R after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1256912Inhibition of human IDH1 R132H mutant expressed in IPTG-induced Escherichia coli BL21 cells assessed as oxidation of NADPH to NADP+ after 5 mins by spectrophotometry2015Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23
Discovery of α-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1.
AID1445702Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1233702Cytotoxicity against human A549 cells assessed as cell viability by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Synthesis and cancer cell growth inhibitory activity of icaritin derivatives.
AID1233701Cytotoxicity against human MDA-MB-435S cells assessed as cell viability by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Synthesis and cancer cell growth inhibitory activity of icaritin derivatives.
AID671764Inhibition of HCV NS3 helicase ATP hydrolysis activity overexpressed in Escherichia coli BL21(DE3) assessed as inhibition of inorganic phosphate release by AM/MG-based colometric analysis in the presence of M13 ssDNA2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification of myricetin and scutellarein as novel chemical inhibitors of the SARS coronavirus helicase, nsP13.
AID1445697Antibacterial activity against methicillin-resistant Staphylococcus aureus DM 21455 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445707Antibacterial activity against methicillin-resistant Staphylococcus aureus DB57964 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445711Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-sensitive Staphylococcus aureus DM4583R2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445716Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-sensitive Staphylococcus aureus ATCC 297372017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID362785Inhibition of human recombinant PDE5A1 expressed in COS7 cells2008Journal of natural products, Sep, Volume: 71, Issue:9
Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
AID1445719Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-resistant Staphylococcus aureus DB579642017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445699Antibacterial activity against methicillin-sensitive Staphylococcus aureus DM4583R after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID428313Reversal of P-gp-mediated multidrug resistance in human MCF7 cells assessed as assessed as increase in intracellular adriamycin accumulation at 5 uM incubated 2 hrs before adriamycin challenge by spectrophotometry2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis and antimultidrug resistance evaluation of icariin and its derivatives.
AID1445703Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 6538 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445721Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-resistant Staphylococcus aureus ATCC 7006992017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445701Antibacterial activity against methicillin-sensitive Staphylococcus aureus DM4299 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445709Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 700699 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445705Antibacterial activity against methicillin-resistant Staphylococcus aureus DB6506 after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445718Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-resistant Staphylococcus aureus DB680042017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445713Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-sensitive Staphylococcus aureus DM42992017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445717Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-resistant Staphylococcus aureus DB65062017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445715Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-sensitive Staphylococcus aureus ATCC 65382017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID428319Inhibition of P-gp in human Caco-2 cells assessed as decrease in efflux permeability from basolateral to apical side at 50 uM after 120 mins2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis and antimultidrug resistance evaluation of icariin and its derivatives.
AID1445712Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-sensitive Staphylococcus aureus DM4400R2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445730Induction of plasma membrane permeability in methicillin-resistant Staphylococcus aureus DM9808R assessed as increase in fluorescence intensity at 12.5 ug/ml measured every 1 sec for 50 mins by SYTOX green dye based fluorimetric assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445700Antibacterial activity against methicillin-sensitive Staphylococcus aureus DM4400R after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1445695Antibacterial activity against methicillin-resistant Staphylococcus aureus DM 9808R after 24 hrs by broth microdilution method2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID1233703Cytotoxicity against African green monkey Vero cells assessed as cell viability by MTT assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Synthesis and cancer cell growth inhibitory activity of icaritin derivatives.
AID428318Inhibition of P-gp in human Caco-2 cells assessed as increase in influx permeability from apical to basolateral side at 50 uM after 120 mins2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Synthesis and antimultidrug resistance evaluation of icariin and its derivatives.
AID1774205Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay2021Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20
Design, Synthesis, and Biological Evaluation of Icaritin Derivatives as Novel Putative DEPTOR Inhibitors for Multiple Myeloma Treatment.
AID1445720Ratio of HC50 for New Zealand white rabbit RBC to MIC for methicillin-resistant Staphylococcus aureus ATCC 433002017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Semisynthetic Flavone-Derived Antimicrobials with Therapeutic Potential against Methicillin-Resistant Staphylococcus aureus (MRSA).
AID671761Inhibition of SARS coronavirus nsP13 helicase activity expressed in Escherichia coli Rosetta assessed inhibition of DNA unwinding activity at 10 uM by FRET assay2012Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
Identification of myricetin and scutellarein as novel chemical inhibitors of the SARS coronavirus helicase, nsP13.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (201)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's17 (8.46)29.6817
2010's123 (61.19)24.3611
2020's61 (30.35)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 33.87

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index33.87 (24.57)
Research Supply Index5.32 (2.92)
Research Growth Index5.41 (4.65)
Search Engine Demand Index47.56 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (33.87)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.50%)5.53%
Reviews5 (2.48%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other196 (97.03%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]