10074-G5

Research use only, not for human use.

A small molecules that disrupts c-Myc-Max heterodimerization.

A small molecules that disrupts c-Myc-Max heterodimerization; binds to and distorts the bHLH-ZIP domain of c-Myc; inhibits the growth of Daudi Burkitt's lymphoma cells and disrupts c-Myc/Max dimerization.

10074-G5 inhibits the growth of Daudi Burkitt's lymphoma cells and disruptes c-Myc/Max dimerization. The IC50 values against Daudi and HL-60 cells are 15.6 and 13.5 μM, respectively. 10074-G5 binds the Myc peptide Myc353-437 with a Kd value of 2.8 μM in the region Arg363-Ile381. 10074-G5 binds in a cavity that is created by a kink (Asp379-Ile381) in the N-terminus of an induced helical domain (Leu370–Arg378).

The plasma half-life of 10074-G5 in mice treated with 20 mg/kg i.v. is 37 min, and peak plasma concentration was 58 μM, which is 10-fold higher than peak tumor concentration.

10074G5

Cell Cycle/DNA Damage

c-Myc

c-Myc

Cancer

——

413611-93-5

332.31288

C18H12N4O3

>98% (HPLC)

DMSO: ≥ 28 mg/mL

O=[N+](C1=CC=C(NC2=CC=CC=C2C3=CC=CC=C3)C4=CNON41)[O-]

2,1,3-Benzoxadiazol-4-amine, N-[1,1'-biphenyl]-2-yl-7-nitro-

(-20℃)

With Ice Pack

≥ 2 years