475957
c-Myc Inhibitor II
The c-Myc Inhibitor II, also referenced under CAS 413611-93-5, controls the biological activity of c-Myc.
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Synonym(s):
c-Myc Inhibitor II, 7-Nitro-N-(2-phenylphenyl)-2,1,3-benzoxadiazol-4-amine, Biphenyl-2-yl-(7-nitrobenzo[1,2,5]oxadiazol-4-ylamine, 10074-G5
Empirical Formula (Hill Notation):
C18H12N4O3
Recommended Products
Quality Level
Assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
deep orange
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
2-8°C
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
General description
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 residues 363 and 381 (KD = 4.4 µM), while 10058-F4 interaction site is located within aa residues 402 through 412 (KD = 13 µM).
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).
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Follis, A.V., et al. 2008. Chem. Biol.15, 1149.
Yin, X., et al. 2003. Oncogene22, 6151.
Sold under license of U.S. Patent 7,026,343.
Yin, X., et al. 2003. Oncogene22, 6151.
Sold under license of U.S. Patent 7,026,343.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Yue-Zhi Lee et al.
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Endothelial dysfunction is prominent in atherosclerosis, hypertension, diabetes, peripheral and cardiovascular diseases, and stroke. Novel therapeutic approaches to these conditions often involve development of tissue-engineered veins with ex vivo expanded endothelial cells. However, high cell number requirements limit these approaches
Ashutosh Singh et al.
The Journal of biological chemistry, 297(1), 100903-100903 (2021-06-23)
c-Myc is a transcription factor that plays a crucial role in cellular homeostasis, and its deregulation is associated with highly aggressive and chemotherapy-resistant cancers. After binding with partner MAX, the c-Myc-MAX heterodimer regulates the expression of several genes, leading to
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