SecinH3

Catalog No.S7685 Batch:S768501

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Technical Data

Formula

C24H20N4O4S
Molecular Weight 460.5 CAS No. 853625-60-2
Solubility (25°C)* In vitro DMSO 92 mg/mL (199.78 mM)
Ethanol 1 mg/mL (2.17 mM)
Water Insoluble
* <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 SecinH3 is a selective cytohesin inhibitor with IC50 of 2.4 μM, 5.4 μM, 5.4 μM, 5.6 μM, 5.6 μM, and 65 μM for hCyh2, hCyh1, mCyh3, hCyh3, drosophila steppke, and yGea2-S7, respectively.
Targets
hCyh2 [1] hCyh1 [1] mCyh3 [1] hCyh3 [1] drosophila steppke [1] View More
2.4 μM 5.4 μM 5.4 μM 5.6 μM 5.6 μM
In vitro In HepG2 cells, SecinH3 inhibits insulin signaling and associated gene expression. [1] SecinH3 also markedly inhibits migration of preadipocyte 3T3-L1 cells. [2] In the A549 cells, SecinH3 results in reduced proliferation by indirectly attenuating EGFR activation, and causes a synergistic antiproliferative effect when used in combination with gefitinib. [3]
In vivo In mice, SecinH3 increases the expression of gluconeogenic genes, reduces the expression of glycolytic, fatty acid and ketone body metabolism genes in the liver, reduces liver glycogen stores, and increases plasma insulin. [1] In mice bearing H460 xenografts, SecinH3 significantly retards tumor growth through its antiproliferative and pro-apoptotic effect. [3]

Protocol (from reference)

Kinase Assay:[1]
  • Aptamer displacement screen

    A library of small molecules screened in duplicate from Comgenex (10000 molecules) in 386 well plates by fluorescence polarization at an excitation wavelength of 485 nm using read-out at 520 nm in a reaction volume of 50 μL at 37° C. The screening buffer is PBS, pH 7.5, 3 mM MgCl2, 100 nM fluorecein-labelled M69 aptamer, 1 μM cytohesin-1 Sec7 at 100 μM compound concentrations.
Cell Assay:[3]
  • Cell lines

    NSCLC A549 and H460 cell lines

  • Concentrations

    ~15 μM

  • Incubation Time

    72 hours

  • Method

    3×103 cells per 96 well are seeded into a clear, flat bottom 96 well plate (TPP). After 24 h the cells are treated with the indicated concentrations of the inhibitors or solvent (final DMSO concentration 0.4%) in RPMI containing 50 ng/mL EGF or IGF-1, respectively. Medium is changed daily for 3 days and cell proliferation is analyzed with a MTT assas as described in the manufacturer’s protocol using a Varioscan microplate reader. All assays are performed at least in triplicates.

Animal Study:[3]
  • Animal Models

    Mice bearing H460 xenografts

  • Dosages

    100 μL 2.5 mM, once daily

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , J Exp Clin Cancer Res, 2017, 36(1):112]

Data from [Data independently produced by , , IUBMB Life, 2018, 71(2):192-199]

Selleck's SecinH3 has been cited by 4 publications

Blocking the cytohesin-2/ARF1 axis by SecinH3 ameliorates osteoclast-induced bone loss via attenuating JNK-mediated IRE1 endoribonuclease activity [ Pharmacol Res, 2022, 185:106513] PubMed: 36252772
Genome-wide CRISPR-Cas9 screening identifies the CYTH2 host gene as a potential therapeutic target of influenza viral infection [ Cell Rep, 2022, 38(13):110559] PubMed: 35354039
SecinH3 Attenuates TDP-43 p.Q331K-Induced Neuronal Toxicity by Suppressing Endoplasmic Reticulum Stress and Enhancing Autophagic Flux [Hu W, et al. IUBMB Life, 2018, 71(2):192-199] PubMed: 30376609
Combined targeting of Arf1 and Ras potentiates anticancer activity for prostate cancer therapeutics. [Lang L, et al. J Exp Clin Cancer Res, 2017, 36(1):112] PubMed: 28830537

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.