Product description
The 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 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM).{30637,30638,30640} 10074-G5 is cytotoxic to c-Myc-overexpressing cells lines with IC50 values of 15.6 and 13.5 µM for Daudi Burkitt lymphoma cells and HL60 promyelocytic leukemia cells, respectively.{30636} 10074-G5 can also interfere with N-Myc/Max interactions (Kd = 19.2 µM for binding the bHLH-Zip of N-Myc), inducing apoptosis in N-Myc amplified neuroblastoma Kelly cells (IC50 = 22.5 µM).{30639}
Specifications
CAS number
413611-93-5
Supplier
Cayman Chemical
Shipping & storage
Shipping condition
Dry Ice
Storage temperature
-20°C

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10074-G5

17408-1

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