EPI-001

• UNSPSC Description:

  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].

• Target Antigen:

  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:

  98.87

• 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 Weight:

  394.89

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  No Development Reported

• CAS Number:

  227947-06-0