EPI-001

EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer[1][2][3].

Product Specifications

CAS Number

[227947-06-0]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Androgen Receptor; Apoptosis; PPAR

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/epi-001.html

Purity

99.34

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

OCC(O)COC1=CC=C(C(C)(C2=CC=C(OCC(O)CCl)C=C2)C)C=C1

Molecular Formula

C21H27ClO5

Molecular Weight

394.89

Precautions

H315, H319, H335

References & Citations

[1]Andersen RJ, et, al. Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor. Cancer Cell. 2010 Jun 15; 17 (6) : 535-46.|[2]Brand LJ, 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. Oncotarget. 2015 Feb 28; 6 (6) : 3811-24.|[3]Mol ED, et, al. EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor. ACS Chem Biol. 2016 Sep 16;11 (9) :2499-505.