EPI-001
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EPI-001是雄激素受体N-末端结构域的小分子抑制剂。EPI-001靶向AR的氨基末端结构域，抑制蛋白-蛋白相互作用，这对于AR转录活性是必需的。雄激素受体（AR）参与介导雄性类固醇的作用。雄激素受体基因的扩增和过表达可导致激素难治性前列腺癌[1]。
体外实验：EPI-001抑制LNCaP细胞中配体依赖性的ARGal4转录活性，在CRPC C4-2细胞系中，EPI-001抑制不依赖于ARGal4的转录活性。在一系列细胞系中，如雄激素敏感前列腺癌、CRPC、LNCAP、C4-2和LAPC4细胞系，经EPI-001处理8和16小时后，AR蛋白的mRNA表达水平降低。EPI-001会剂量依赖性地抑制PCA/CRPC细胞生长[2]。
在体实验：在非阉割的成熟小鼠中，EPI-001的静脉注射显著地减少了良性前列腺的重量，抑制前列腺癌异种移植物的生长。EPI-001引起CRPC肿瘤消退。在LNCaP异种移植雄性小鼠中，静脉注射EPI-001 2周后，肿瘤体积小于对照组的一半[3]。
参考文献：
Andersen R J, Mawji N R, Wang J, et al. Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor[J]. Cancer cell, 2010, 17(6): 535-546.
Brand L J, Olson M E, Ravindranathan P, et al. EPI-001 is a selective peroxisome proliferator-activated receptor-gamma modulator with inhibitory effects on androgen receptor expression and activity in prostate cancer[J]. Oncotarget, 2015, 6(6): 3811.
Sadar M D. Small molecule inhibitors targeting the “achilles' heel” of androgen receptor activity[J]. Cancer research, 2011, 71(4): 1208-1213.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 394.89 |
| Cas No. | 227947-06-0 |
| Formula | C21H27ClO5 |
| Solubility | insoluble in H2O; ≥14.46 mg/mL in EtOH; ≥19.75 mg/mL in DMSO with ultrasonic |
| Chemical Name | 3-(4-(2-(4-(3-chloro-2-hydroxypropoxy)phenyl)propan-2-yl)phenoxy)propane-1,2-diol |
| SDF | Download SDF |
| Canonical SMILES | CC(C1=CC=C(OCC(O)CCl)C=C1)(C2=CC=C(OCC(O)CO)C=C2)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
相关生物数据
