A cell-permeable pyrazolopyrimidine-carboxamide that selectively inhibits c-Myc-Max dimer DNA binding activity (IC50=23uM) by preventing c-Myc-Max heterodimer formation, while affecting Max, Jun, C/EBPa homodimers, or Jun-Fos heterodimer DNA binding only at much higher concentrations (IC50=>54uM). Shown to selectively inhibit c-Myc-Max-dependent transcription (by 77% against E-Box promoter-driven reporter transcription at 10uM), cancer proliferation, and anchorage-independent colony formation (Effective conc. 10-20uM).
Formula:C₁₇H₁₁F₃N₄OS₂
Primary Target:a-helical dimerization motifs of c-Myc/Max factors
Primary Target IC50:IC50 = 23 and 54uM for c-Myc/Max and Max/Max dimerization
Secondary target:a-helical dimerization motifs of Max/Max factors
Molecular Weight:408.4
Solubility:DMSO (100mg/ml clear, yellow solution)
Storage and Stability:May be stored at 4°C for short-term only. Long-term storage is recommended at -20°C. Stable for 1 year after receipt. Protect from light when in solution. For maximum recovery of product, centrifuge the original vial prior to removing the cap.