10074-G5

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). 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. 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).Formal Name: N-[1,1'-biphenyl]-2-yl-7-nitro-2,1,3-benzoxadiazol-4-amine. CAS Number: 413611-93-5. Molecular Formula: C18H12N4O3. Formula Weight: 332.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml, Ethanol: 2 mg/ml. lambdamax: 232, 327, 467 nm. SMILES: O=[N+](C(C1=NON=C12)=CC=C2NC3=CC=CC=C3C4=CC=CC=C4)[O-]. InChi Code: InChI=1S/C18H12N4O3/c23-22(24)16-11-10-15(17-18(16)21-25-20-17)19-14-9-5-4-8-13(14)12-6-2-1-3-7-12/h1-11,19H. InChi Key: KMJPYSQOCBYMCF-UHFFFAOYSA-N.