Genistein

别名: NPI 031L 中文名称：金雀异黄酮，染料木素

目录号：S1342 Purity: 99.88%

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

CAS: 446-72-0

规格	价格	库存
10mM (1mL in DMSO)	736.52	现货
25mg	569.08	现货
100mg	1417.83	现货
更大包装有超大折扣
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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

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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(PMID)
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

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K_i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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考文献
https://pubmed.ncbi.nlm.nih.gov/3106339/ https://pubmed.ncbi.nlm.nih.gov/2153378/ https://pubmed.ncbi.nlm.nih.gov/12421816/ https://pubmed.ncbi.nlm.nih.gov/11880592/ https://pubmed.ncbi.nlm.nih.gov/16808622/ + 展开

参考文献

https://pubmed.ncbi.nlm.nih.gov/3106339/
https://pubmed.ncbi.nlm.nih.gov/2153378/
https://pubmed.ncbi.nlm.nih.gov/12421816/

https://pubmed.ncbi.nlm.nih.gov/11880592/
https://pubmed.ncbi.nlm.nih.gov/16808622/

+ 展开

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

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

体内溶解配方批次：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
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	2.700mg/ml (9.99mM)	以 1 mL 工作液为例,取50μL54mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
澄清溶液	5% DMSO 1 95% Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	0.340mg/ml (1.26mM)	以1 mL工作液为例，取50μL 6.8mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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，注：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：取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：取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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* 必填项

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