compound 3i (666-15)

Catalog No.S8846 Batch:S884601

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Technical Data

Formula

C33H31Cl2N3O5
Molecular Weight 620.52 CAS No. 1433286-70-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (161.15 mM)
Ethanol 3 mg/mL (4.83 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml
5% DMSO 95% Corn oil
2.5mg/ml
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    6- to 8-week old BALB/c nude mouse inoculated subcutaneously at the right flank with MDA-MB-468 cells

  • Dosages

    10 mg/kg

  • Administration

    IP

Selleck's compound 3i (666-15) has been cited by 15 publications

The PKA-CREB1 axis regulates coronavirus proliferation by viral helicase nsp13 association [ J Virol, 2024, 98(4):e0156523] PubMed: 38445884
The delta subunit of the GABAA receptor is necessary for the GPT2-promoted breast cancer metastasis [ Theranostics, 2023, 13(4):1355-1369] PubMed: 36923530
Inhibiting the glycerophosphodiesterase EDI3 in ER-HER2+ breast cancer cells resistant to HER2-targeted therapy reduces viability and tumour growth [ J Exp Clin Cancer Res, 2023, 42(1):25] PubMed: 36670508
MLK4 promotes glucose metabolism in lung adenocarcinoma through CREB-mediated activation of phosphoenolpyruvate carboxykinase and is regulated by KLF5 [ Oncogenesis, 2023, 12(1):35] PubMed: 37407566
MLK4 promotes glucose metabolism in lung adenocarcinoma through CREB-mediated activation of phosphoenolpyruvate carboxykinase and is regulated by KLF5 [ Oncogenesis, 2023, 12(1):35] PubMed: 37407566
Paradoxical Induction of ALOX15/15B by Cortisol in Human Amnion Fibroblasts: Implications for Inflammatory Responses of the Fetal Membranes at Parturition [ Int J Mol Sci, 2023, 24(13)10881] PubMed: 37446059
LIM1 contributes to the malignant potential of endometrial cancer [ Front Oncol, 2023, 13:1082441] PubMed: 36969081
pH sensing controls tissue inflammation by modulating cellular metabolism and endo-lysosomal function of immune cells [ Nat Immunol, 2022, 10.1038/s41590-022-01231-0] PubMed: 35668320
Downregulation of IL-8 and IL-10 by the Activation of Ca2+-Activated K+ Channel KCa3.1 in THP-1-Derived M2 Macrophages [ Int J Mol Sci, 2022, 23(15)8603] PubMed: 35955737
Activation of cAMP Signaling in Response to α-Phellandrene Promotes Vascular Endothelial Growth Factor Levels and Proliferation in Human Dermal Papilla Cells [ Int J Mol Sci, 2022, 23(16)8959] PubMed: 36012223

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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