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.
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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 |
++++
EGFRT790M, IC50: 0.79 nM EGFRL858R/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 |
++++
EGFRdel19 T790M C797S, IC50: 0.2 nM |
99%+ | |||||||||||||||||
EGFR-IN-7 |
++++
EGFRd746-750/T790M/C797S, IC50: 0.26 nM EGFRL858R/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。 |
靶点 |
|
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]. |
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 | ||
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 |
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 |