Genistein | NPI 031L;CI-75610;BIO300;SIPI-9764-I;PTI-G-4660;G-2535;Genistein, BIO-300;NSC 36586 | 金雀异黄酮 | Plant Standard | Tyrosine / EGF Receptor Protein Kinase Inhibitor | EGFR | PTK

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染料木素 /Genistein 98%

货号：A107459 同义名： 金雀异黄酮 / NPI 031L;CI-75610

Genistein has multiple biological functions. It can inhibit several tyrosine kinases (IC50 of 0.6 μM for EGFR), inhibits DNA topoisomerase-II and activation of PPARs. Genistein is a phytoestrogen which has selective estrogen receptor modulator properties.

Genistein 化学结构
CAS号：446-72-0

Genistein 3D分子结构
CAS号：446-72-0

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Genistein 纯度/质量文件产品仅供科研

货号：A107459 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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EGFR 亚型比较

产品名称	EGFR/ErbB1 ↓ ↑	ErbB3 ↓ ↑	ErbB4 ↓ ↑	HER2/ErbB2 ↓ ↑	mutant EGFR ↓ ↑	其他靶点	纯度
WZ-3146	++++ EGFR (E746_A750), IC50: 2 nM EGFR (E746_A750/T790M), IC50: 14 nM						99%+
Daphnetin	+ EGFR, IC50: 7.67 μM					PKA,PKC	99%+
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		98%+
PD168393	++++ EGFR, IC50: 0.70 nM						99%+
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		99%+
Norcantharidin	✔						98%
CL-387785	++++ EGFR, IC50: 370 pM						98%
WHI-P154	+++ EGFR, IC50: 4 nM					Src,VEGFR	99%+
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	98%
AG 555	+ EGFR, IC50: 0.7 μM						99%+
AG 494	+ EGFR, IC50: 1.2 μM						99%+
AG-556	+ EGFR, IC50: 5 μM						98%
RG13022	+ EGFR, IC50: 4 μM						99%+
Tyrphostin RG 14620	✔						99%+
Vandetanib	+ EGFR, IC50: 500 nM						99%+
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		99%+
AZD3759	++++ EGFR (WT), IC50: 0.3 nM EGFR (L858R), IC50: 0.2 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						99%+
Saracatinib	+++ EGFR, IC50: 5 nM EGFR (L861Q), IC50: 4 nM						99%+
AG1557	✔						98%
Rociletinib	++ EGFR (L858R/T790M), Ki: 21.5 nM EGFR (wt), Ki: 303.3 nM						99%+
AG490	+ EGFR, IC50: 0.1 μM						98%
Cetuximab	++++ EGFR, Kd: 0.39 nM						99%+
Osimertinib	++ L858R/T790M EGFR, IC50: 11.44 nM WT EGFR, IC50: 12.92 nM						99%
Osimertinib mesylate	✔						98% (Content MsOH 15.2-18.2%)
Chrysophanol	✔					mTOR	98%
PD153035	++++ EGFR, Ki: 5.2 pM						99%+
Olmutinib	✔					BTK	99%+
WZ4002	++++ EGFR (L858R/T790M), IC50: 8 nM EGFR (L858R), IC50: 2 nM						99%+
Icotinib	+++ EGFR, IC50: 5 nM						98+%
Desmethyl Erlotinib HCl	++++ EGFR, IC50: 2 nM						98%
Cyasterone	✔						99%+
PP 3	+ EGFR tyrosine kinase, IC50: 2.7 μM						98%
WZ8040	✔						99%+
(-)-Epigallocatechin Gallate	✔						99%
AG 18	+ EGFR, IC50: 35 μM						99%+
O-Desmethyl gefitinib	++ EGFR, IC50: 36 nM						98%
Falnidamol	✔						99%+
AZ-5104	++++ EGFR (L858R), IC50: 6 nM EGFR (L861Q) , IC50: <1 nM		+++ ErbB4, IC50: 7 nM			BRK	99%+
Butein	✔						99%+
Genistein	✔						98%
SU5214	+ EGFR, IC50: 36.7 μM						99%+
Naquotinib	✔						99%+
Gefitinib	++ EGFR, IC50: 15.5 nM				+ EGFR (858R/T790M), IC50: 823.3 nM		99%+
Theliatinib	+++ WT EGFR, IC50: 3 nM				++ EGFR T790M/L858R, IC50: 22 nM		98+%
Lazertinib	++++ L858R/T790M EGFR, IC50: 2 nM WT EGFR, IC50: 76 nM				++++ Del19/T790M, IC50: 1.7 nM		99%+
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						99%+
MTX-211	✔					PI3K	99%+
(E)-AG 99	✔						99%+
Licochalcone D	✔					Caspase,PARP	97%
Zipalertinib	+++ EGFR WT, IC50: 8 nM EGFR (L861Q), IC50: 4.1 nM		+++ HER4, IC50: 4 nM		++++ EGFR L858R, IC50: 2 nM EGFR(d746-750), IC50: 1.4 nM		97%
JND3229	+++ EGFR WT, IC50: 6.8 nM				++ EGFR L858R/T790M, IC50: 30.5 nM		99%+
Firmonertinib mesylate	✔						99%+
Tyrphostin AG30	✔						99%+
EGFR-IN-12	++ EGFR, IC50: 21 nM						99%+
Mobocertinib	✔						99%+
(Rac)-JBJ-04-125-02	✔						99%
(S)-Sunvozertinib	✔						99%+
BLU-945	✔						99%+
Poziotinib	+++ HER1, IC50: 3.2 nM		++ HER4, IC50: 23.5 nM	+++ HER2, IC50: 5.3 nM			98%
TAK-285	++ EGFR/HER1, IC50: 23 nM		+ HER4, IC50: 260 nM	++ HER2, IC50: 17 nM			99%+
ARRY-380 analog				✔			99%+
Canertinib	++++ EGFR, IC50: 1.5 nM			+++ ErbB2, IC50: 9.0 nM			99%+
Dacomitinib	+++ EGFR, IC50: 6.0 nM		+ ErbB4, IC50: 73.7 nM	+ ErbB2, IC50: 45.7 nM			98%
EGFR/ErbB-2/ErbB-4 inhibitor-2			+ ErbB4, IC50: 1.91 μM	+ ErbB2, IC50: 0.08 μM			99%+
(E/Z)-CP-724714				++ HER2/ErbB2, IC50: 10 nM			98+%
Lapatinib	++ EGFR, IC50: 10.8 nM		+ ErbB4, IC50: 367 nM	+++ ErbB2, IC50: 9.2 nM			99%+
AEE788	++++ EGFR, IC50: 2 nM		+ HER4/ErbB4, IC50: 160 nM	+++ HER2/ErbB2, IC50: 6 nM		c-Fms	98+%
AV-412 free base	++++ EGFR, IC50: 0.75 nM			++ ErbB2, IC50: 19 nM	++++ EGFR^T790M, IC50: 0.79 nM EGFR^L858R/T790M, IC50: 0.51 nM		99%+
Neratinib	+ EGFR, IC50: 92 nM			+ HER2, IC50: 59 nM		Src	99%+
BMS-599626	++ HER1, IC50: 20 nM		+ HER4, IC50: 190 nM	++ HER2, IC50: 30 nM			99+%
Tucatinib				+++ ErbB2, IC50: 8 nM			99%+
Allitinib	++++ EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Pelitinib	+ EGFR, IC50: 38.5 nM			+ ErbB2, IC50: 1.255 μM		Src,Raf	99%+
Sapitinib	+++ EGFR, IC50: 4 nM	+++ ErbB3, IC50: 4 nM		+++ ErbB2, IC50: 3 nM			99%+
CUDC-101	+++ EGFR, IC50: 2.4 nM			++ HER2, IC50: 15.7 nM		HDAC	99%+
Varlitinib	+++ ErbB1, IC50: 7 nM			++++ ErbB2, IC50: 2 nM			99%+
Afatinib dimaleate	++++ EGFR (L858R/T790M), IC50: 0.4 nM EGFR (wt), IC50: 0.5 nM			++ HER2, IC50: 14 nM			99%+
Canertinib dihydrochloride	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			98%
Allitinib tosylate	++++ EGFR, IC50: 0.5 nM EGFR (T790M/L858R), IC50: 12 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Tyrphostin AG 528	+ EGFR, IC50: 4.9 μM			+ HER2, IC50: 2.1 μM			98%
Afatinib	++++ EGFR (wt), IC50: 0.5 nM EGFR (L858R), IC50: 10 nM		++++ ErbB4, IC50: 1 nM	++ HER2, IC50: 14 nM			99%
Pyrotinib dimaleate	++ EGFR, IC50: 0.013 μM			++ HER2, IC50: 0.038 μM			98%
Epertinib HCl	++++ EGFR, IC50: 1.48 nM		+++ HER4, IC50: 2.49 nM	+++ HER2, IC50: 7.15 nM			98%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			98%
ALK-IN-1					++ EGFR(del19), IC50: 36.8 nM EGFR(C797S/del19), IC50: 138.6 nM	ALK	99%+
Brigatinib					+ EGFR(C797S/T790M/del19), IC50: 67.2 nM EGFR(del19), IC50: 39.9 nM	FLT3,ALK	98%
Avitinib					++++ EGFR L858R/T790M, IC50: 0.18 nM	BTK	99%+
EAI045					✔		99%+
Almonertinib					✔		99%+
BI-4020					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		99%+
EGFR-IN-7					++++ EGFR^{d746-750/T790M/C797S}, IC50: 0.26 nM EGFR^L858R/T790M, IC50: 0.19 nM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Genistein 生物活性

靶点

EGFR/ErbB1
Topo II

描述

Genistein is an isoflavone present in soy and is known to have multiple molecular effects, such as the inhibition of inflammation, promotion of apoptosis, and modulation of steroidal hormone receptors and metabolic pathways^[3]. Genistein is the natural isoflavone and a phytoestrogen with a broad range of pharmacological properties, such as tyrosine and topoisomerase inhibition. It also induces apoptosis and cell proliferation inhibition, differentiates cancer cells. Added health benefits include the reduction of osteoporosis by suppressing osteoclasts and lymphocyte functions, decreased the risk of cardiovascular attacks and relieved postmenopausal problems^[4]. Retardation of atherogenic activity and increasing the antioxidant defense of a cell has been attributed to genistein while as it has also been reported that genistein possesses suppressive effects on both the cell-mediated and humoral components of the adaptive immune system. In addition, genistein has its prominent role in preventing the DNA damage. Genistein confers a better protection to ischemic conditions thereby giving a significant cardioprotection^[5]. Gensitein possesses cancer related enzyme-inhibitory effect and substantially inhibits skin carcinogenesis and cutaneous aging induced by ultraviolet (UV) light in mice and photodamage in humans. The anticancer, anti-inflammatory, cardio-protective and enzyme-inhibitory effects of genistein might be related to their antioxidant activities^[6].

Genistein 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
293T cells		Function assay		Displacement of [3H]17beta-estradiol from recombinant human ERbeta expressed in 293T cells, IC50=0.0013 μM	16219463
3T3 cells		Cytotoxic assay		Cytotoxic effect on 3T3 cells, IC50=24 μM	8201603
A431 cells	50 to 75 uM	Function assay	36 h	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
ANN-1 cells		Cytotoxic assay		Cytotoxic effect on v-abl transformed murine ANN-1 cells, IC50=8 μM	8201603

Genistein 参考文献

[1]Jalili C, Ahmadi S, et al. Effect of Genistein on reproductive parameter and serum nitric oxide levels in morphine-treated mice. Int J Reprod Biomed (Yazd). 2016 Feb;14(2):95-102.

[2]Akiyama T, Ishida J, et al. Genistein, a specific inhibitor of tyrosine-specific protein kinases. J Biol Chem. 1987 Apr 25;262(12):5592-5.

[3]Mukund V, Mukund D, Sharma V, Mannarapu M, Alam A. Genistein: Its role in metabolic diseases and cancer. Crit Rev Oncol Hematol. 2017 Nov;119:13-22

[4]Jaiswal N, Akhtar J, Singh SP; Badruddeen, Ahsan F. An Overview on Genistein and its Various Formulations. Drug Res (Stuttg). 2019 Jun;69(6):305-313

[5]Ganai AA, Farooqi H. Bioactivity of genistein: A review of in vitro and in vivo studies. Biomed Pharmacother. 2015 Dec;76:30-8

[6]Rahman Mazumder MA, Hongsprabhas P. Genistein as antioxidant and antibrowning agents in in vivo and in vitro: A review. Biomed Pharmacother. 2016 Aug;82:379-92

Genistein 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.70mL

0.74mL

0.37mL

18.50mL

3.70mL

1.85mL

37.00mL

7.40mL

3.70mL

Genistein 技术信息

CAS号	446-72-0
分子式	C₁₅H₁₀O₅
分子量	270.237

别名	金雀异黄酮 ;NPI 031L;CI-75610;BIO300;SIPI-9764-I;PTI-G-4660;G-2535;Genistein, BIO-300;NSC 36586
运输	蓝冰

存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(388.55 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

293T cells		Function assay		Displacement of [3H]17beta-estradiol from recombinant human ERbeta expressed in 293T cells, IC50=0.0013 μM	16219463
3T3 cells		Cytotoxic assay		Cytotoxic effect on 3T3 cells, IC50=24 μM	8201603
A431 cells	50 to 75 uM	Function assay	36 h	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
ANN-1 cells		Cytotoxic assay		Cytotoxic effect on v-abl transformed murine ANN-1 cells, IC50=8 μM	8201603
HEK293 cells		Function assay		Antagonist activity at human recombinant LXRbeta expressed in HEK293 cells by luciferase reporter gene assay, IC50=22 μM	18343126
HEK293 cells		Function assay		Antagonist activity at human recombinant LXRalpha expressed in HEK293 cells by luciferase reporter gene assay, IC50=31 μM	18343126
HeLa cells		Function assay		Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor beta, EC50=0.0041 μM	11906280
human A549 cells		Cytotoxic assay	72 h	Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50=43.09 μM	21129977
human AGS cells		Cytotoxic assay	72 h	Cytotoxicity against human AGS cells after 72 hrs by MTT assay, IC50=41.67 μM	21129977
human BT20 cell		Proliferation assay		Antiproliferative activity against human BT20 cell line by MTT assay, IC50=46 μM	16789737
human BxPC3 cell		Proliferation assay		Antiproliferative activity against human BxPC3 cell line by MTT assay, IC50=30 μM	16789737
human DU145 cells		Cytotoxic assay	72 h	Cytotoxicity against human DU145 cells after 72 hrs by MTT assay, IC50=47.29 μM	21129977
human HCT116 cells		Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=34.9 μM	21129977
human HL60 cells		Function assay	24 h	Antileukemic activity against human HL60 cells after 24 hrs by clonogenic assay, LC50=6.3 μM	18163589
human Ishikawa cells		Function 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=0.51 μM	12502307
human LNCAP cells		Cytotoxic assay	72 h	Cytotoxicity against human LNCAP cells after 72 hrs by SRB assay, IC50=30.65 μM	21129977
human LoVo cells		Cytotoxic assay	72 h	Cytotoxicity against human LoVo cells after 72 hrs by MTT assay, IC50=15.88 μM	21129977
human MCF7 cells		Cytotoxic assay	48 h	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=1 μM	20813524
human MCF7 cells		Proliferation assay		Antiproliferative activity against estrogen receptor expressing human MCF7 cells, GI50=10 μM	19818612
human MCF7 cells		Function assay	6 h	Inhibition of phorbol ester-induced ornithine decarboxylase in human MCF7 cells after 6 hrs, IC50=26 μM	10075742
human MCF7 cells	0.1-20 μM	Function assay	4 days	Stimulation of growth in human MCF7 cells at 0.1 to 20 uM after 4 days by MTT assay	25078314
human MCF7 cells	20-100 μM	Growth inhibition assay	4 days	Growth inhibition in human MCF7 cells at 20 to 100 uM after 4 days by MTT assay	25078314
human MDA-kb2 cells		Function assay		Agonist activity at androgen receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay	19592245
human MOLT3 cells		Function assay	24 h	Antileukemic activity against human MOLT3 cells after 24 hrs by clonogenic assay, LC50=7.5 μM	18163589
human MOLT3 cells		Growth inhibition assay	48 h	Growth inhibition of human MOLT3 cells after 48 hrs	18163589
human PC3 cells		Proliferation assay	48 h	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=42.658 μM	21513275
human Raji cells		Function assay	24 h	Antileukemic activity against human Raji cells after 24 hrs by clonogenic assay, LC50=13.7 μM	18163589
human SKBR3 cells	50 to 75 uM	Function assay	36 h	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
human T47D cells		Function 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	15787436
human U937 cells		Proliferation assay	72 h	Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay, IC50=48 μM	17158054
HUVE12 cells		Function assay		Reversal of hydrogen peroxide-induced LDH activity in human HUVE12 cells	18068980
K562 cells		Growth inhibition assay	5 days	Growth inhibition of K562 cells by XTT assay after 5 days, IC50=17.56 μM	17411092
MDCK cells		Function assay		Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=6.9 μM	21354800
mouse L1210 cells		Function assay	24 h	Antileukemic activity against mouse L1210 cells after 24 hrs by clonogenic assay, LC50=6.5 μM	18163589
mouse RAW264.7 cells		Function assay	24 h	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=19.1 μM	21288727
NHEM cells		Function assay	72 h	Inhibition of melanin synthesis in NHEM cells assessed as [14C]thiouracil incorporation after 72 hrs by liquid scintillation counting, IC50=29.2 μM	19132934
NIH3T3 cells		Function assay		Agonist activity at CFTR-deltaF508 mutant expressed in NIH3T3 cells assessed as increase in forskolin-stimulated current, EC50=4.4 μM	18595696
RAW 264 cells		Function assay	24 h	Inhibition of 1 ug/ml LPS-stimulated TNFalpha accumulation in RAW 264 cells after 24 hrs, IC50=18.1 μM	17320246
WiDr human colon cells		Cytotoxic assay		Cytotoxic effect on WiDr human colon cells, IC50=27.7 μM	8201603

染料木素 /Genistein 98%

Genistein 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Genistein 质控信息

Genistein 生物活性

Genistein 细胞研究

Genistein 参考文献

Genistein 实验方案

Genistein 技术信息

最近浏览的产品

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EGFR/ErbB1
Topo II

染料木素 /Genistein 98%

Genistein 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Genistein 质控信息

Genistein 生物活性

Genistein 细胞研究

Genistein 参考文献

Genistein 实验方案

Genistein 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Genistein 纯度/质量文件产品仅供科研