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.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EPI-001 is a small-molecule inhibitor of androgen receptor N-terminal domain. EPI-001 could target the amino terminal domain of the AR and inhibit the protein-protein interactions which are necessary for AR transcriptional activity. The androgen receptor (AR) is involved in mediating the actions of male sex steroids. Amplification and over-expression of androgen receptor gene may result in hormone-refractory prostate cancer .
In vitro: EPI-001 inhibited the ligand-dependent ARGal4 transcriptional activity in LNCaP cells and the ligand-independent ARGal4 transcriptional activity in the CRPC C4-2 cell line. In a panel of cell lines, EPI-001 treatment decreased the mRNA expression level of AR protein after 8 and 16 h treatment, such as androgen sensitive PCa, CRPC, LNCap, C4-2, and LAPC4 cell line. EPI-001 dose-dependently inhibited the PCa/CRPC cell growth .
In vivo: Intravenous injection of EPI-001 significantly reduced the weight of benign prostates and blocked the growth of prostate cancer xenograft from noncastrated mature mice. EPI-001 caused tumor regression of CRPC. In male mice bearing LNCaP xenografts, after treated with EPI- 001 by i.v. injection for 2 weeks, the tumor size was less than half of the control group .
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|
|Solubility||≥19.75mg/mL in DMSO with ultrasonic|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|