VPC-70063 is a potent Myc-Max inhibitor with an IC50 value of 8.9 μM for Myc-Max transcriptional activity inhibition. VPC-70063 reduces UBE2C promotor activity and AR-V7 levels, and induces PARP cleavage. VPC-70063 induces apoptosis and blocks Myc-Max interactions with DNA. VPC-70063 can be used for researching anticancer.
VPC-70063 (25 μM; 96 h) shows Myc-Max transcriptional activity inhibition of 106% and Myc-Max/UBE2C downstream pathway inhibition of 94%[1].VPC-70063 (6.25-25 μM, 48 h) causes apoptosis of LNCaP cells as indicated by cleavage of PARP[1].VPC-70063 (0-500 μM; 0-600 s) disrupts the interaction of Myc-Max with DNA in a dose dependent manner[1].
References:
[1]. Carabet LA, et al. Computer-aided drug discovery of Myc-Max inhibitors as potential therapeutics for prostate cancer. Eur J Med Chem. 2018 Dec 5;160:108-119.