Home Protein Tyrosine Kinase EGFR inhibitor Genistein

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Genistein EGFR inhibitor

Cat.No.S1342

Genistein, a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM.
Genistein EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 270.24

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Quality Control

Batch: Purity: 99.88%
99.88

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BxPC3 Proliferation assay Antiproliferative activity against human BxPC3 cell line by MTT assay, IC50=30 μM 16789737
BT20 Proliferation assay Antiproliferative activity against human BT20 cell line by MTT assay, IC50=46 μM 16789737
ANN-1 Cytotoxic assay Cytotoxic effect on v-abl transformed murine ANN-1 cells, IC50=8μM 8201603
breast carcinoma cells Cytotoxic assay Cytotoxic effect on MCF-7 human breast carcinoma cells, IC50=15.1μM 8201603
3T3 Cytotoxic assay Cytotoxic effect on 3T3 cells, IC50=24μM 8201603
colon cells Cytotoxic assay Cytotoxic effect on WiDr human colon cells, IC50=27.7μM 8201603
Hepa1clc7 Cytotoxicity assay 72 hrs Cytotoxicity against mouse Hepa1clc7 cells after 72 hrs, IC50=11μM 10075742
MCF7 Function assay 6 hrs Inhibition of phorbol ester-induced ornithine decarboxylase in human MCF7 cells after 6 hrs, IC50=26μM 10075742
3T3/A31 Cytotoxicity assay 1 to 100 ug/mL 72 hrs Cytotoxicity against BALB/c mouse cloned 3T3/A31 cells at 1 to 100 ug/mL after 72 hrs by nigrosin assay 10096863
SH-SY5Y Function assay Agonist activity in transcriptional activation assay in SH-SY5Y neuroblastoma cells expressing Estrogen receptor beta, EC50=0.0017μM 11906280
HeLa Function assay Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor beta., EC50=0.0041μM 11906280
HeLa Function assay Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor alpha., EC50=0.048μM 11906280
Ishikawa Estrogenic assay 4 days Estrogenic activity in human Ishikawa cells assessed as induction of alkaline phosphatase activity after 4 days by para-nitrophenol release assay, IC50=0.51μM 12502307
Hepa-1c1c7 Function assay Induction of NADPH:quinone reductase in mouse Hepa-1c1c7 cells assessed as drug level required to double enzyme activity by MTT assay, CD=22.9μM 14510590
Hepa-1c1c7 Function assay Inhibition of mouse Hepa-1c1c7 cells by MTT assay, IC50=45.2μM 14510590
T47D Estrogenic assay Estrogenic activity in human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol by alamar blue assay, Activity=0.001μM 15787436
MCF7 Estrogenic assay Estrogenic activity in human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol by alamar blue assay, Activity=0.003μM 15787436
T47D Estrogenic assay Estrogenic activity in human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol by alamar blue assay, Activity=0.009μM 15787436
MCF7 Estrogenic assay Estrogenic activity in human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol by alamar blue assay, Activity=0.013μM 15787436
293T Function assay Displacement of [3H]17beta-estradiol from recombinant human ERbeta expressed in 293T cells, IC50=0.0013μM 16219463
293T Function assay Displacement of [3H]17beta-estradiol from recombinant human ERalpha expressed in 293T cells, IC50=0.0294μM 16219463
Vero Cytotoxicity assay Cytotoxicity against african green monkey Vero cells, IC50=32.9μM 16441066
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay, IC50=48μM 17158054
RAW 264 Function assay 24 hrs Inhibition of 1 ug/ml LPS-stimulated TNFalpha accumulation in RAW 264 cells after 24 hrs, IC50=18.1μM 17320246
K562 Growth inhibition assay 5 days Growth inhibition of K562 cells by XTT assay after 5 days, IC50=17.56μM 17411092
HUVE12 Function assay Reversal of hydrogen peroxide-induced LDH activity in human HUVE12 cells 18068980
HL60 Antileukemic assay 24 hrs Antileukemic activity against human HL60 cells after 24 hrs by clonogenic assay, LC50=6.3μM 18163589
L1210 Antileukemic assay 24 hrs Antileukemic activity against mouse L1210 cells after 24 hrs by clonogenic assay, LC50=6.5μM 18163589
MOLT3 Antileukemic assay 24 hrs Antileukemic activity against human MOLT3 cells after 24 hrs by clonogenic assay, LC50=7.5μM 18163589
MOLT3 Growth inhibition assay 48 hrs Growth inhibition of human MOLT3 cells after 48 hrs, IG50=12.7μM 18163589
Raji Antileukemic assay 24 hrs Antileukemic activity against human Raji cells after 24 hrs by clonogenic assay, LC50=13.7μM 18163589
HL60 Growth inhibition assay 48 hrs Growth inhibition of human HL60 cells after 48 hrs, IG50=18.2μM 18163589
L1210 Growth inhibition assay 24 hrs Growth inhibition of mouse L1210 cells after 24 hrs, IG50=18.5μM 18163589
Raji Growth inhibition assay 48 hrs Growth inhibition of human Raji cells after 48 hrs, IG50=18.6μM 18163589
KG1a Growth inhibition assay 48 hrs Growth inhibition of human KG1a cells after 48 hrs, IG50=23μM 18163589
L1210 Function assay 1 to 20 uM 24 hrs Induction of p15CDKN2B re-expression in mouse L1210 cells at 1 to 20 uM after 24 hrs by RT-PCR 18163589
HEK293 Function assay Antagonist activity at human recombinant LXRbeta expressed in HEK293 cells by luciferase reporter gene assay, IC50=22μM 18343126
HEK293 Function assay Antagonist activity at human recombinant LXRalpha expressed in HEK293 cells by luciferase reporter gene assay, IC50=31μM 18343126
NIH3T3 Function assay Agonist activity at CFTR-deltaF508 mutant expressed in NIH3T3 cells assessed as increase in forskolin-stimulated current, EC50=4.4μM 18595696
NHEM Function assay 72 hrs Inhibition of melanin synthesis in NHEM cells assessed as [14C]thiouracil incorporation after 72 hrs by liquid scintillation counting, IC50=29.2μM 19132934
RAW264.7 Function assay Inhibition of LPS-induced TNFalpha release in mouse RAW264.7 cells pretreated 1 hr before LPS challenge by enzyme immunoassay, IC50=26.5μM 19278854
MDA-kb2 Function assay Agonist activity at androgen receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150=4.4μM 19592245
MDA-kb2 Function assay Agonist activity at glucocorticoid receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150=4.4μM 19592245
MCF7 Antiproliferative assay Antiproliferative activity against estrogen receptor expressing human MCF7 cells, GI50=10μM 19818612
MDA-MB-436 Antiproliferative assay Antiproliferative activity against estrogen receptor expressing human MDA-MB-436 cells, GI50=17μM 19818612
FRT Function assay Binding affinity to CFTR deltaF508 mutant expressed in FRT cells coexpressing halide sensitive YFP-H148Q/I152L mutant protein by iodide influx assay, Kd=16.7μM 19880323
T47D Estrogenic assay 96 hrs Estrogenic activity in human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol after 96 hrs by alamar blue assay, Activity=0.01μM 19928832
MCF7 Estrogenic assay 96 hrs Estrogenic activity in human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol after 96 hrs by alamar blue assay, Activity=0.01μM 19928832
MCF7 Estrogenic assay Estrogenic activity in luciferase transfected human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol by luciferase reporter gene assay, Activity=0.01μM 19928832
MCF7 Estrogenic assay Estrogenic activity in luciferase transfected human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol by luciferase reporter gene assay, Activity=0.01μM 19928832
T47D Estrogenic assay Estrogenic activity in luciferase transfected human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol by luciferase reporter gene assay, Activity=0.01μM 19928832
T47D Estrogenic assay 96 hrs Estrogenic activity in human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol after 96 hrs by alamar blue assay, Activity=0.08μM 19928832
MCF7 Estrogenic assay 96 hrs Estrogenic activity in human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol after 96 hrs by alamar blue assay, Activity=0.11μM 19928832
T47D Estrogenic assay Estrogenic activity in luciferase transfected human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 100 pM estradiol by luciferase reporter gene assay, Activity=0.6μM 19928832
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 24 hrs by Griess reagent, IC50=26μM 20363145
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=1μM 20813524
LoVo Cytotoxicity assay 72 hrs Cytotoxicity against human LoVo cells after 72 hrs by MTT assay, IC50=15.88μM 21129977
LNCAP Cytotoxicity assay 72 hrs Cytotoxicity against human LNCAP cells after 72 hrs by SRB assay, IC50=30.65μM 21129977
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=34.9μM 21129977
AGS Cytotoxicity assay 72 hrs Cytotoxicity against human AGS cells after 72 hrs by MTT assay, IC50=41.67μM 21129977
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50=43.09μM 21129977
DU145 Cytotoxicity assay 72 hrs Cytotoxicity against human DU145 cells after 72 hrs by MTT assay, IC50=47.29μM 21129977
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production treated 2 hrs before LPS challenge measured after 24 hrs by ELISA, IC50=19.1μM 21288727
MDCK Function assay Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=6.9μM 21354800
MCF-7 MX Function assay Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=8.8μM 21354800
NCI-ADR-RES Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=16.9824μM 21513275
MCF12A Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=21.8776μM 21513275
NCI-ADR-RES Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=26.9154μM 21513275
MCF12A Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=30.1995μM 21513275
NCI-ADR-RES Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50=32.3594μM 21513275
MCF12A Antiproliferative assay 48 hrs Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50=32.3594μM 21513275
LNCAP Antiproliferative assay 48 hrs Antiproliferative activity against human LNCAP cells expressing androgen receptor incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50=38.9045μM 21513275
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against androgen receptor-deficient human PC3 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50=42.6579μM 21513275
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50=45.7088μM 21513275
FRT Function assay 24 hrs Binding affinity to CFTR F508 deletion mutant expressed in forskolin-stimulated FRT cells assessed as increase in iodine influx measured as YFP quenching rate after 24 hrs by fluorescence assay, Kd=9.4μM 21568323
MCF7 Antiestrogenic assay 1 to 20 uM 48 hrs Antiestrogenic activity in human ER-positive MCF7 cells assessed as inhibition of 17beta estradiol-induced secreted alkaline phosphatase activity at 1 to 20 uM after 48 hrs by phospha-light reporter chemiluminescence assay 21800859
Jurkat T Apoptosis assay 36 hrs Induction of apoptosis in human Jurkat T cells overexpressing Neo after 36 hrs by flow cytometry 22197393
FRT Function assay Potentiation activity at human CFTR delta F508 mutant-mediated iodine flux expressed in rat FRT cells coexpressing fluorescent protein YFP-H148Q/1152L by fluorescence assay, EC50=7μM 22281185
Human Huh7.5.1 Antiviral assay 72 hrs Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay, EC50=14.4μM 22445328
CHO Function assay Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells, Ki=2.96μM 23571415
CHO Function assay pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells, IC50=3.89045μM 23571415
CHO Function assay Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells, Ki=5μM 23571415
CHO Function assay pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells, IC50=9.12011μM 23571415
HuH7 Antiplasmodial assay 24 hrs Antiplasmodial activity against liver sporozoite stage of Plasmodium berghei ANKA expressing GFP infected in human HuH7 cells assessed as inhibition of parasite development after 24 hrs by qRT-PCR analysis, IC50=20μM 24125849
SKBR3 Cell cycle assay 50 to 75 uM 36 hrs Cell cycle arrest in human SKBR3 cells assessed as decrease in accumulation at G0/G1 phase at 50 to 75 uM after 36 hrs by propidium iodide staining-based flow cytometric analysis 24456004
A431 Cell cycle assay 50 to 75 uM 36 hrs Cell cycle arrest in human A431 cells assessed as decrease in accumulation at G0/G1 phase at 50 to 75 uM after 36 hrs by propidium iodide staining-based flow cytometric analysis 24456004
A431 Cell cycle assay 50 to 75 uM 36 hrs Cell cycle arrest in human A431 cells assessed as accumulation at G2/M phase at 50 to 75 uM after 36 hrs by propidium iodide staining-based flow cytometric analysis relative to control 24456004
A431 Apoptosis assay 50 to 75 uM 72 hrs Induction of apoptosis in human A431 cells overexpressing ErbB in complete medium assessed as late apoptotic/necrotic cells at 50 to 75 uM after 72 hrs by annexin V-FITC/7-AAD staining-based flow cytometric analysis 24456004
MCF7 Growth inhibition assay 0.1 to 20 uM 4 days Stimulation of growth in human MCF7 cells at 0.1 to 20 uM after 4 days by MTT assay 25078314
MCF7 Growth inhibition assay 20 to 100 uM 4 days Growth inhibition in human MCF7 cells at 20 to 100 uM after 4 days by MTT assay 25078314
RAW264.7 Function assay 26 uM Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as nitrites level at 26 uM by Griess method (Rvb = 6.4 +/- 0.5 uM), Activity=6.1μM 25127153
RAW264.7 Function assay 6.5 uM Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as nitrites level at 6.5 uM by Griess method (Rvb = 6.4 +/- 0.5 uM), Activity=6.3μM 25127153
RAW264.7 Function assay 13 uM Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse RAW264.7 cells assessed as nitrites level at 13 uM by Griess method (Rvb = 6.4 +/- 0.5 uM), Activity=6.3μM 25127153
J774A1 Function assay 6.5 uM Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse J774A1 cells assessed as nitrites level at 6.5 uM by Griess method (Rvb = 16.5 +/- 1.4 uM), Activity=13.4μM 25127153
J774A1 Function assay 13 uM Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse J774A1 cells assessed as nitrites level at 13 uM by Griess method (Rvb = 16.5 +/- 1.4 uM), Activity=13.8μM 25127153
J774A1 Function assay 26 uM Inhibition of nitric oxide production in LPS/IFNgamma-stimulated mouse J774A1 cells assessed as nitrites level at 26 uM by Griess method (Rvb = 16.5 +/- 1.4 uM), Activity=14.5μM 25127153
HEK293 Function assay Inhibition of EGFR (unknown origin) expressed in HEK293 cells assessed as decrease in phosphorylation by chemiluminescence assay, IC50=25.12μM 25205190
Sf9 Function assay Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil, IC50=30μM 25406944
LNCAP Cytotoxicity assay 3 days Cytotoxicity against human androgen-dependent LNCAP cells assessed as inhibition of cell viability after 3 days by WST-1 cell proliferation assay, IC50=37.4μM 26341135
insect cells Function assay 10 mins Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells preincubated for 10 mins followed by addition of kynuramine as substrate, IC50=3.9μM 27575476
insect cells Function assay 10 mins Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells preincubated for 10 mins followed by addition of benzylamine as substrate, IC50=4.1μM 27575476
insect cells Function assay 40 mins Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells assessed as decrease in arbitrary light units preincubated for 40 mins followed by addition of luciferin derivative substrate measured after 2 hrs by MAO-Glow assay, IC50=6.8μM 27575476
insect cells Function assay 40 mins Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells assessed as decrease in arbitrary light units preincubated for 40 mins followed by addition of luciferin derivative substrate measured after 2 hrs by MAO-Glow assay, IC50=9.7μM 27575476
RAW264.7 Antiosteoporotic assay 4 to 5 days Antiosteoporotic activity in mouse RAW264.7 cells assessed as inhibition of RANKL-induced osteoclast differentiation after 4 to 5 days by TRAP assay, IC50=11.4μM 28169537
SK-MEL-2 Cytotoxicity assay 48 hrs Cytotoxicity against human SK-MEL-2 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=36μM 28654265
MML1 Cytotoxicity assay 48 hrs Cytotoxicity against human MML1 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=42μM 28654265
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=43μM 28654265
LN229 Cytotoxicity assay 48 hrs Cytotoxicity against human LN229 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=44μM 28654265
NCI-H460 Cytotoxicity assay 48 hrs Cytotoxicity against human NCI-H460 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=47μM 28654265
T47D Cytotoxicity assay 48 hrs Cytotoxicity against human T47D cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50=48μM 28654265
HepG2 Function assay 1 hr Inhibition of IL-6-Induced STAT3 activation (unknown origin) expressed in human HepG2 cells expressing pSTAT3-luciferase pre-incubated for 1 hr before IL-6 stimulation for 6 hrs by luciferase reporter gene assay, IC50=24.8μM 29140705
UOCB1 Antiproliferative assay 72 hrs Antiproliferative activity against human UOCB1 cells after 72 hrs by CelTiter-Glo assay, EC50=35.6958μM 29407975
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LNCAP Antiproliferative assay Antiproliferative activity against human LNCAP cells, IC50=10μM 29456113
LNCAP Antiproliferative assay 72 hrs Antiproliferative activity against human LNCAP cells after 72 hrs by MTS assay, IC50=24μM 29456113
LNCAP Antiproliferative assay 72 hrs Antiproliferative activity against human LNCAP cells after 72 hrs in presence of enzalutamide by MTS assay, IC50=31.7μM 29456113
LNCAP Function assay 2.5 uM 24 hrs Inhibition of HDAC6/HSP90 in human LNCAP cells assessed as downregulation of AR protein level at 2.5 uM after 24 hrs by Western blot method 29456113
BV2 Antiinflammatory assay Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production, IC50=28.4μM 29482940
MDA-MB-231/beta41 Estrogenic assay 18 hrs Estrogenic activity at ERbeta (unknown origin) expressed in human MDA-MB-231/beta41 cells after 18 hrs by renilla luciferase reporter gene assay, EC50=0.0024μM 29641206
Ishikawa Estrogenic assay 96 hrs Estrogenic activity at ERalpha in human Ishikawa cells assessed as induction of alkaline phosphatase activity using p-nitrophenol as substrate treated for 96 hrs followed by substrate addition by spectrophotometric method, EC50=0.24μM 29641206
HEK293 Function assay 48 hrs Agonist activity at human ER-beta transfected in HEK293 cells after 48 hrs by luciferase reporter gene assay, EC50=0.01995μM ChEMBL
HEK293 Function assay 48 hrs Agonist activity at human ER-alpha transfected in HEK293 cells after 48 hrs by luciferase reporter gene assay, EC50=0.50119μM ChEMBL
HT-29 Growth inhibition assay Growth inhibition of Homo sapiens (human) HT-29 cells by MTT assay, GI=4.11μM ChEMBL
HL60 Growth inhibition assay Growth inhibition of Homo sapiens (human) HL60 cells by MTT assay, GI=4.82μM ChEMBL
SGC7901 Growth inhibition assay Growth inhibition of Homo sapiens (human) SGC7901 cells by MTT assay, GI=5.78μM ChEMBL
HL60 Function assay Competitive inhibition of GLUT1 in human HL60 cells assessed as reduction in 2-[1,2-3H]deoxy-D-glucose uptake measured for 30 secs by double reciprocal plot analysis, Ki=7μM ChEMBL
CHO Function assay Competitive inhibition of GLUT1 (unknown origin) expressed in CHO cells assessed as reduction in 2-[1,2-3H]deoxy-D-glucose uptake measured for 30 secs by double reciprocal plot analysis, Ki=7μM ChEMBL
3T3L1 Function assay Inhibition of GLUT4 in mouse 3T3L1 cells assessed as reduction in insulin-stimulated 2-deoxy-D-[14C]glucose uptake, IC50=20μM ChEMBL
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Solubility

In vitro
Batch:

DMSO : 54 mg/mL (199.82 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 270.24 Formula

C15H10O5

 Storage (From the date of receipt)
CAS No. 446-72-0 Download SDF Storage of Stock Solutions

Synonyms NPI 031L Smiles C1=CC(=CC=C1C2=COC3=CC(=CC(=C3C2=O)O)O)O

Mechanism of Action

Targets/IC50/Ki
EGFR
topo II
In vitro

Genistein is an ATP competitive inhibitor. This compound inhibits tyrosine phosphorylation in isolated enzyme and receptor preparations and in whole cells including platelets, lymphocytes and a variety of cultured cells. It also inhibits EGF-stimulated phosphorylation in cultured cells as well as inhibition of Topo II (topoisomerase II). This chemical inhibits EGF-stimulated tyrosine phosphorylation in cultured A431 epidermoid carcinoma cells. Inhibition is competitive with ATP and noncompetitive with substrate. It blocks the mitogenic effect mediated by EGF and thrombin on NIH-3T3 cells. This compound also acts as an agonist at the GPR30 receptor and binds to PPARγ and estrogen receptors. It also binds to PPARγ, acting as an agonist at this receptor with Ki of 5.7 μM.

In vivo

Genistein has chemopreventive effects on breast, prostate, and other endocrine-dependent tumors in adult animals. This compound in the diet reduced the incidence of poorly differentiated prostatic adenocarcinomas in a dose-dependent manner and down-regulated androgen receptor, estrogen receptor-alpha, epidermal growth factor receptor, and extracellular signal-regulated kinase-1 but not estrogen receptor-beta and transforming growth factor-alpha mRNA expressions. Dietary genistein protects against mammary and prostate cancers by regulating specific sex steroid receptors and growth factor signaling pathways. This chemical combined with prostate tumor irradiation causes greater inhibition of primary tumor growth and increases control of spontaneous metastasis to para-aortic lymph nodes, increasing mouse survival. Paradoxically, treatment with this compound alone increases metastasis to lymph nodes.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11880592/
  • [5] https://pubmed.ncbi.nlm.nih.gov/16808622/

Applications

Methods Biomarkers Images PMID
Western blot PPARγ / C/EBPα / αP2 p-ERK Foxo3 CIP2A / PARP / Cleaved PARP / Caspase-3 / Cleaved Caspase-3 p-AKT / AKT DNMT-1 / DNMT-3a / DNMT-3b
S1342-WB1
18384126
Immunofluorescence ER-β / pS87 ER-β
S1342-IF2
25931004

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05073523 Completed
Healthy
Chalmers University of Technology
 September 27 2021 Not Applicable
NCT04650555 Completed
Acute Radiation Syndrome
Humanetics Corporation|United States Department of Defense|Joint Warfighter Medical Research Program
 December 8 2020 Phase 1
NCT01982578 Completed
Alzheimer''s Disease
Fundación para la Investigación del Hospital Clínico de Valencia|University of Valencia
 September 1 2017 Not Applicable
NCT02499861 Completed
Cancer
St. Justine''s Hospital
 July 2015 Phase 1|Phase 2
NCT01628471 Completed
Non Small Cell Lung Cancer
Uman Pharma|DSM Nutritional Products Inc.|MDEIE Ministry Québec Government|INRS-Institut Armand Frappier Université du Québec
 November 2012 Phase 1|Phase 2

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Signaling Pathway Map