A cell-permeable pyrazolopyrimidine-carboxamide that selectively inhibits c-Myc-Max dimer DNA binding activity (IC₅₀ = 23 µM) by preventing c-Myc-Max heterodimer formation, while affecting Max, Jun, C/EBPα homodimers, or Jun-Fos heterodimer DNA binding only at much higher concentrations (IC₅₀ = 54 µM for Max-Max dimer and IC₅₀ > >54 µM for the rest). Shown to selectively inhibit c-Myc-Max-dependent transcription (by 77%, 31%, and 19%, respectively, against E-Box, AP-1, and SRE promoter-driven reporter transcription with 10 µM inhibitior), anchorage-independent colony formation (By 40% and 2%, respectively, against c-Myc or v-Src transformed Rat1a cells with 15 µM inhibitor) and proliferation (Effective conc. 10-20 µM in Raji, MCF-7, and U2OS cultures), but not c-Myc-independent proliferation of PC-12 cells (by <10% at 20 µM).

Cell permeable: yes

IC₅₀ = 23 and 54 µM for c-Myc/Max and Max/Max dimerization

Primary Target
α-helical dimerization motifs of c-Myc/Max factors

Reversible: yes

Secondary Target
α-helical dimerization motifs of Max/Max factors

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Kiessling, A., et al. 2006. Chem. Biol.13, 745.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany