- Product Name10074-G5
- Brief DescriptionInhibitors
- Purification97.22%
- Biological ActivityThe c-Myc oncoprotein is overexpressed in many tumors and is essential for maintaining the proliferation of transformed cells. To function as a transcription factor, c-Myc must dimerize with Max?via?the basic helix-loop-helix leucine zipper protein (bHLH-ZIP) domains in each protein. 10074-G5 is a c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd?= 2.8 ?M), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50?= 146 ?M). 10074-G5 is cytotoxic to c-Myc-overexpressing cells lines with IC50?values of 15.6 and 13.5 ?M for Daudi Burkitt lymphoma cells and HL60 promyelocytic leukemia cells, respectively.?10074-G5 can also interfere with N-Myc/Max interactions (Kd?= 19.2 ?M for binding the bHLH-Zip of N-Myc), inducing apoptosis in N-Myc amplified neuroblastoma Kelly cells (IC50?= 22.5 ?M)
- Target Namec-Myc inhibitor
- CAS No. 413611-93-5
- Calculated MW 332.32
- Formulation C18H12N4O3
- Storage 3 years -20˚C powder;2 years -80˚C in solvent;
