compound 3i (666-15)

Catalog No.S8846

compound 3i (666-15) Chemical Structure

Molecular Weight(MW): 620.52

Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.

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Biological Activity

Description Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.
Targets
CREB [1]
()
81 nM
In vitro

666-15 could potently inhibit cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI50 for 666-15 is 73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibit robust activity as well with GI50 of 0.47 and 0.31 μM. 666-15 inhibits CREB’s transcription activity in living cells independent of direct CREB or CBP binding interaction[1].

In vivo

In an in vivo MDA-MB-468 xenograft model, 666-15 completely suppresses the tumor growth without overt toxicity. Preliminary toxicity studies show that intraperitoneal (ip) injection of 10 mg/kg of 666-15 is well tolerated in mice[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: HEK 293T cells
  • Concentrations: 0.05, 0.1, 0.5 μM
  • Incubation Time: --
  • Method:

    HEK 293T cells are treated with different concentrations of 666-15 followed by treatment with forskolin. Then the relative mRNA level of Nurr1/NR4A2 is determined by qRT-PCR analysis.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: 6- to 8-week old BALB/c nude mouse inoculated subcutaneously at the right flank with MDA-MB-468 cells
  • Formulation: 1% N-methylpyrrolidone (NMP), 5% Tween-80 in H2O
  • Dosages: 10 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (161.15 mM)
Ethanol 3 mg/mL (4.83 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 620.52
Formula

C33H31Cl2N3O5

CAS No. 1433286-70-4
Storage powder
in solvent
Synonyms N/A

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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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Epigenetic Reader Domain Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID