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NFPA 704
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2
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N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine C화학적 특성, 용도, 생산
일반 설명
A cell-permeable benzoxadiazole compound that is shown to preferentially disrupt the interactions of c-Myc-Max, Mad1-Max, and Myf5-HEB, over those of 31 other pairs of HLH-, ZIP-, and HLH-ZIP-containing proteins. Similarly to 10058-F4 (Cat. No. 475956), 10074-G5 is shown to selectively inhibit the c-Myc-dependent growth of rat fibroblast cell line TGR1 and effectively suppress c-Myc-dependent transcription activity. Binding studies using various mutated and truncated c-Myc constructs reveal that 10074-G5 targets c-Myc helix-1 region between aa 363 and 381 (KD = 4.4 μM), while 10058-F4 interaction site is located within aa residues 402 through 412 (KD = 13 μM).
Biochem/physiol Actions
10074-G5 is a c-Myc/Max interaction inhibitor. The c-Myc oncoprotein and its partner Max are intrinsically disordered (ID) monomers that undergo coupled folding and binding upon heterodimerization. 10074-G5, similarly to 10058-F4 (#F3680), specifically inhibits this interaction by binding to c-Myc, thus preventing C-Myc specific DNA binding and target genes regulation. 10074-G5 (2.8 microM) is slightly more potent that 10058-F4 (5.2 microM). It was discovered that 10074-G5 binds to a different specific binding site (region) of C-Myc than 10054-F4. Thus, the compound may become desirable for probing different interactions.
N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine 준비 용품 및 원자재
원자재
준비 용품
N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine 공급 업체
