10074-G5

For research use only.

Catalog No.S8426

1 publication

10074-G5 Chemical Structure

CAS No. 413611-93-5

10074-G5 is a c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM).

Selleck's 10074-G5 has been cited by 1 publication

Purity & Quality Control

Choose Selective Myc Inhibitors

Biological Activity

Description 10074-G5 is a c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM).
Targets
c-Myc [1]
(Cell-free assay)
2.8 μM(Kd)
In vitro

10074-G5 binds to and distorts the bHLH-ZIP domain of c-Myc, thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity. In vitro, 10074-G5 inhibits the growth of Daudi Burkitt's lymphoma cells and disrupts c-Myc/Max dimerization. Daudi cells accumulates 10074-G5, and the highest intracellular concentration is observed at 6 h. 10074-G5 inhibits c-Myc/Max dimerization in Daudi cells by approximately 75% at 4 h, and this inhibition is maintained through 24 h of incubation. Total c-Myc protein expression also decreases, and after 24 h exposure to 10 μM 10074-G5, c-Myc protein expression decreases approximately 40% compared with vehicle-treated control. 10074-G5 is cytotoxic in vitro against Daudi and HL-60 cells, which overexpress c-Myc [2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Daudi cells MX;DfZRwfG:6aXPpeJkh[XO|YYm= M172W|MhfG9iNTDkZZl{ NUH3OnM4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTGG3ZHmgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiMzD0c{A2KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVExKM7ebR?= NHT5bWkzOzF5N{K1Oi=>
HL60 cells M4HnTmN6fG:2b4jpZ4l1gSCjc4PhfS=> NEH5WW8{KHSxIEWg[IF6ew>? M{X3eWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhNPjBiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhOyC2bzC1JIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUOwJO69VQ>? NFfCOHczOzF5N{K1Oi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
MYCN; 

PubMed: 24859015     


Western blot analysis of MYCN expression in SK-N-BE(2) cells treated for 48 hours with the indicated concentrations of 10058-F4. Membranes were probed with antibodies recognizing MYCN and GAPDH. The blots are representative from three independent experiments.

HER2 / p-AKT / AKT / HOXB7 ; 

PubMed: 26180042     


Immunoblot analysis of HER2, P-AKT, and HOXB7 in BT474 cells after treatment with 10 uM 10058-F4, 100 ug/ml of trastuzumab, or a combination of 10058-F4 and trastuzumab.

24859015 26180042
In vivo The plasma half-life of 10074-G5 in mice treated with 20 mg/kg i.v. is 37 min, and peak plasma concentration is 58 μM, which is 10-fold higher than peak tumor concentration. The lack of antitumor activity probably is caused by the rapid metabolism of 10074-G5 to inactive metabolites, resulting in tumor concentrations of 10074-G5 insufficient to inhibit c-Myc/Max dimerization. Plasma 10074-G5 peak concentration (Cmax) of 58.5 ± 2.7 nmol/ml is observed at 5 min after intravenous administration of 20 mg/kg to mice bearing Daudi xenografts, 10074-G5 concentration in plasma declines rapidly. Except for lung, liver, and fat, tissue concentrations of 10074-G5 are lower than those of plasma at all time points[2].

Protocol

Cell Research:[2]
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  • Cell lines: Daudi cells
  • Concentrations: 10 μM
  • Incubation Time: 0, 1, 3, 6, or 24 h
  • Method: Daudi cells (3 × 108 cells in logarithmic growth) are incubated for 0, 1, 3, 6, or 24 h in 3 ml of complete medium containing 10 μM 10074-G5. After incubation, cells are harvested, split into two samples of 1.5 ml each, and overlaid in microcentrifuge tubes containing 0.5 ml of silicon oil. The tubes are centrifuged at 12,000g for 4 min. After centrifugation, the top 1 ml of medium is removed and stored in cryovials at −70°C until analysis. The remaining medium and silicon oil are carefully removed without disturbing the cell pellets. The sides of the tubes are cleaned with cotton-tipped applicators, and the cell pellets are stored at −70°C until analysis.
    (Only for Reference)
Animal Research:[2]
- Collapse
  • Animal Models: Specific-pathogen-free, female C.B-17 SCID mice
  • Dosages: 20 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 60 mg/mL (180.55 mM)
Ethanol 10 mg/mL warmed (30.09 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 332.31
Formula

C18H12N4O3

CAS No. 413611-93-5
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC=C(C=C1)C2=CC=CC=C2NC3=CC=C(C4=NON=C34)[N+](=O)[O-]

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Myc Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID