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VPC-70063

Names

[ CAS No. ]:
13571-44-3

[ Name ]:
VPC-70063

Biological Activity

[Description]:

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[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> PARP
Signaling Pathways >> Apoptosis >> c-Myc
Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

[Target]

IC50: 8.9 μM (Myc-Max)[1]


[In Vitro]

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]. Western Blot Analysis[1] Cell Line: LNCaP cells Concentration: 6.25 μM, 12.5 μM and 25 μM Incubation Time: 48 h Result: Induced PARP cleavage.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C16H12F6N2S

[ Molecular Weight ]:
378.34


Related Compounds