413611-93-5 Usage
Uses
Used in Oncology:
N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine is used as a c-Myc inhibitor for the treatment of tumors with overexpressed c-Myc oncoprotein. By suppressing c-Myc's transcriptional activity, it can potentially inhibit tumor growth and progression in various types of cancer.
Used in Drug Development:
In the pharmaceutical industry, N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine is used as a lead compound for the development of novel therapeutics targeting c-Myc-dependent cancers. Its selective interaction with the c-Myc helix-1 region makes it a valuable starting point for designing more potent and specific inhibitors.
Used in Research:
In the field of molecular biology and cancer research, N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine serves as a valuable tool for studying the role of c-Myc in cancer and its interaction with other proteins. N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine can be used to investigate the mechanisms underlying c-Myc-mediated tumorigenesis and to identify potential therapeutic targets for cancer treatment.
Biological Activity
10074-g5 is a c-myc inhibitor [1].c-myc is a bhlh-zip transcription factor involved in cell cycle progression, cellular growth and metabolism, differentiation, and apoptosis. overexpression of c-myc has been identified in numerous cancers, including prostate, pancreatic, lung, breast, and colon cancers, b-cell lymphoma, and leukemias. alterations in c-myc have been associated with cancer aggressiveness and poor treatment prognosis. inhibition of c-myc is an attractive pharmacological approach in the development of new anticancer treatments. inactivation of c-myc rapidly results in cell-cycle arrest, apoptosis, tumor vascular degeneration, redifferentiation of tumor cells, and ultimately tumor regression [1].the ic50 values of 10074-g5 against daudi cells and hl-60 cells were 15.6 ± 1.5 μm and 13.5 ± 2.1 μm, respectively. 10074-g5 (10 μm) inhibited c-myc/max dimerization and decreased total c-myc protein expression. in c.b-17 scid mice bearing daudi xenografts, treatment with 10074-g5, (20 mg/kg i.v., for 10 consecutive days) significantly inhibited tumor growth with no effects on body weight.
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.
references
[1] clausen d m, guo j, parise r a, et al. in vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-g5, a novel small-molecule inhibitor of c-myc/max dimerization[j]. journal of pharmacology and experimental therapeutics, 2010, 335(3): 715-727.
Check Digit Verification of cas no
The CAS Registry Mumber 413611-93-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,1,3,6,1 and 1 respectively; the second part has 2 digits, 9 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 413611-93:
(8*4)+(7*1)+(6*3)+(5*6)+(4*1)+(3*1)+(2*9)+(1*3)=115
115 % 10 = 5
So 413611-93-5 is a valid CAS Registry Number.
413611-93-5Relevant academic research and scientific papers
POTENT ANALOGUES OF THE C-MYC INHIBITOR 10074-G5 WITH IMPROVED CELL PERMEABILITY
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Paragraph 0078; 0079, (2014/10/16)
The present invention relates compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell. The compounds exhibit increased inhibitory activity against c-Myc relative to the known c-Myc inhibitor small-molecule benzofurazan N-([1,1′-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine (10074-G5).
Pharmacophore identification of c-Myc inhibitor 10074-G5
Yap, Jeremy L.,Wang, Huabo,Hu, Angela,Chauhan, Jay,Jung, Kwan-Young,Gharavi, Robert B.,Prochownik, Edward V.,Fletcher, Steven
supporting information, p. 370 - 374 (2013/02/23)
A structure-activity relationship (SAR) study of the c-Myc (Myc) inhibitor 10074-G5 (N-([1,1′-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4- amine, 1) - which targets a hydrophobic domain of the Myc oncoprotein that is flanked by arginine residues - was executed in order to determine its pharmacophore. Whilst the 7-nitrobenzofurazan was found to be critical for inhibitory activity, the ortho-biphenyl could be replaced with a para-carboxyphenyl group to furnish the new inhibitor JY-3-094 (3q). Around five times as potent as the lead with an IC50 of 33 μM for disruption of the Myc-Max heterodimer, JY-3-094 demonstrated excellent selectivity over Max-Max homodimers, with no apparent effect at 100 μM. Importantly, the carboxylic acid of JY-3-094 improves the physicochemical properties of the lead compound, which will facilitate the incorporation of additional hydrophobicity that might enhance Myc inhibitory activity further still.
