Genistein

别名: NPI 031L 中文名称:金雀异黄酮,染料木素

Genistein是一种来源于大豆的植物雌激素,是一种高特异性的蛋白酪氨酸激酶(PTK) 的抑制剂,在NIH-3T3细胞中通过EGF或者胰岛素介导而抑制有丝分裂,IC50分别为12μM和19 μM。

Genistein Chemical Structure

Genistein Chemical Structure

CAS: 446-72-0

规格 价格 库存 购买数量
10mM (1mL in DMSO) 736.52 现货
25mg 569.08 现货
100mg 1417.83 现货
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产品质控

批次: S134202 DMSO]54 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false 纯度: 99.88%
99.88

Genistein相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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
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
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
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
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
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
K562 Growth inhibition assay 5 days Growth inhibition of K562 cells by XTT assay after 5 days, IC50=17.56μM 17411092
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
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay, IC50=48μM 17158054
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
MCF7 Function assay 6 hrs Inhibition of phorbol ester-induced ornithine decarboxylase in human MCF7 cells after 6 hrs, IC50=26μM 10075742
Hepa1clc7 Cytotoxicity assay 72 hrs Cytotoxicity against mouse Hepa1clc7 cells after 72 hrs, IC50=11μM 10075742
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
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
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
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
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
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
Jurkat T Apoptosis assay 36 hrs Induction of apoptosis in human Jurkat T cells overexpressing Neo after 36 hrs by flow cytometry 22197393
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
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
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
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
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
HUVE12 Function assay Reversal of hydrogen peroxide-induced LDH activity in human HUVE12 cells 18068980
Vero Cytotoxicity assay Cytotoxicity against african green monkey Vero cells, IC50=32.9μM 16441066
293T Function assay Displacement of [3H]17beta-estradiol from recombinant human ERalpha expressed in 293T cells, IC50=0.0294μM 16219463
293T Function assay Displacement of [3H]17beta-estradiol from recombinant human ERbeta expressed in 293T cells, IC50=0.0013μM 16219463
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
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 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 10 pM estradiol by alamar blue assay, Activity=0.001μM 15787436
Hepa-1c1c7 Function assay Inhibition of mouse Hepa-1c1c7 cells by MTT assay, IC50=45.2μM 14510590
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
HeLa Function assay Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor alpha., EC50=0.048μM 11906280
HeLa Function assay Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor beta., EC50=0.0041μM 11906280
SH-SY5Y Function assay Agonist activity in transcriptional activation assay in SH-SY5Y neuroblastoma cells expressing Estrogen receptor beta, EC50=0.0017μM 11906280
colon cells Cytotoxic assay Cytotoxic effect on WiDr human colon cells, IC50=27.7μM 8201603
3T3 Cytotoxic assay Cytotoxic effect on 3T3 cells, IC50=24μM 8201603
breast carcinoma cells Cytotoxic assay Cytotoxic effect on MCF-7 human breast carcinoma cells, IC50=15.1μM 8201603
ANN-1 Cytotoxic assay Cytotoxic effect on v-abl transformed murine ANN-1 cells, IC50=8μM 8201603
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
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
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
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 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
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
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
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
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
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
BV2 Antiinflammatory assay Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production, IC50=28.4μM 29482940
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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生物活性

产品描述 Genistein是一种来源于大豆的植物雌激素,是一种高特异性的蛋白酪氨酸激酶(PTK) 的抑制剂,在NIH-3T3细胞中通过EGF或者胰岛素介导而抑制有丝分裂,IC50分别为12μM和19 μM。
靶点
EGFR [1] topo II [1]
体外研究(In Vitro)
体外研究活性

Genistein是一个ATP竞争性抑制剂。在离体酶,受体制剂和包括血小板、淋巴球的整个细胞以及各种各样人工培养的细胞中,Genistein抑制酪氨酸磷酸化。Genistein也会抑制人工培养细胞中EGF受激的磷酸化作用,并且也会抑制Topo II (拓扑异构酶 II)。Genistein抑制人工培养的A431表皮样癌细胞中EGF受激的酪氨酸磷酸化。抑制作用与ATP竞争,而不与基底竞争。[1] Genistein阻断NIH-3T3 细胞中EGF,胰岛素和凝血酶介导的促有丝分裂作用。[2] Genistein也充当GPR30受体的激动剂,结合于PPARγ和雌激素受体。Genistein也结合于PPARγ,作为该受体的激动剂,其Ki为 5.7 μM。[3]

实验图片 检测方法 检测指标 实验图片 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 18384126
Immunofluorescence ER-β / pS87 ER-β 25931004
体内研究(In Vivo)
体内研究活性

Genistein对成年动物的乳腺癌,前列腺癌和其它内分泌依赖性肿瘤具有预防作用。Genistein在饮食中剂量依赖性减少了低分化前列腺癌的发病率,下调了雄性激素受体,雌激素受体-α,孕激素受体,表皮生长因子受体,胰岛素样生长因子-I和胞外信号调节激酶-1,但不影响雌激素受体-β和转化生长因子-α的mRNA的表达。膳食genistein可以通过调节特定性激素受体和生长因子信号通路预防乳腺癌和前列腺癌。[4] Genistein与前列腺肿瘤辐射结合更加抑制了原发性肿瘤的生长,并且增加了对其自发性转移到主动脉旁淋巴结的控制,提高了小鼠存活率。奇怪的是,Genistein单独治疗增加了其到淋巴结的转移。[5]

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

化学信息&溶解度

分子量 270.24 分子式

C15H10O5

CAS号 446-72-0 SDF Download Genistein SDF
Smiles C1=CC(=CC=C1C2=COC3=CC(=CC(=C3C2=O)O)O)O
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 54 mg/mL ( (199.82 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 4 mg/mL (14.8 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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