N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine
- CAS No.
- 413611-93-5
- Chemical Name:
- N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine
- Synonyms
- 10074-g;10074-G5;10074G5;10074 G5;c-Myc Inhibitor II;10074-G5 >=98% (HPLC);c-Myc Inhibitor II - CAS 413611-93-5 - Calbiochem;N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine;Biphenyl-2-yl-(7-nitrobenzo[1,2,5]oxadiazol-4-yl)amine;N-(2-Biphenylyl)-4-amino-7-nitrobenzo[c][1,2,5]oxadiazole;N-[1,1′-Biphenyl-2-yl]-7-nitro-2,1,3-Benzoxadiazol-4-amine
- CBNumber:
- CB92582970
- Molecular Formula:
- C18H12N4O3
- Molecular Weight:
- 332.31
- MDL Number:
- MFCD00576774
- MOL File:
- 413611-93-5.mol
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS06 |
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Signal word | Danger | |||||||||
Hazard statements | H301-H315-H319-H335 | |||||||||
Precautionary statements | P261-P301+P310-P305+P351+P338 | |||||||||
Hazard Codes | T | |||||||||
Risk Statements | 25-36/37/38 | |||||||||
Safety Statements | 26-45 | |||||||||
RIDADR | UN 2811 6.1 / PGIII | |||||||||
WGK Germany | 3 | |||||||||
NFPA 704 |
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N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine price More Price(19)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | G3798 | 10074-G5 ≥98% (HPLC) | 413611-93-5 | 5mg | $120 | 2024-03-01 | Buy |
Sigma-Aldrich | 475957 | c-Myc Inhibitor II | 413611-93-5 | 10mg | $126 | 2023-06-20 | Buy |
Cayman Chemical | 17408 | 10074-G5 ≥98% | 413611-93-5 | 1mg | $32 | 2024-03-01 | Buy |
Cayman Chemical | 17408 | 10074-G5 ≥98% | 413611-93-5 | 5mg | $70 | 2024-03-01 | Buy |
Sigma-Aldrich | G3798 | 10074-G5 ≥98% (HPLC) | 413611-93-5 | 25mg | $492 | 2024-03-01 | Buy |
N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine Chemical Properties,Uses,Production
Uses
N-[1,1''-Biphenyl]-2-yl-7-nitro-2,1,3-benzoxadiazol-4-amine is a c-Myc inhibitor that suppresses its transcriptional activity.c-Myc is an oncoprotein often found overexpressed in various tumors.
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 363 and 381 (KD = 4.4 μM), while 10058-F4 interaction site is located within aa residues 402 through 412 (KD = 13 μM).
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.
N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
SHANGHAI T&W PHARMACEUTICAL CO., LTD. | +86-021-61551413 +8618813727289 | contact@trustwe.com | China | 5738 | 58 |
Tianjin Xinshengjiahe Science & Technology Development Co,.Ltd | +86-86-22-87899925 +86-8618522618860 | 18522618860@163.com | China | 694 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Shanghai Boyle Chemical Co., Ltd. | 021-50182298 021-50180596 | sales@boylechem.com | China | 2210 | 55 |
Tianjin heowns Biochemical Technology Co., Ltd. | 400 638 7771 | sales@heowns.com | China | 14443 | 57 |
View Lastest Price from N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
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2019-12-24 | N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine
413611-93-5
|
US $1.00 / g | 1g | 99% | 20kg | Career Henan Chemical Co |
- N-2-Biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-aMine
413611-93-5
- US $1.00 / g
- 99%
- Career Henan Chemical Co