SecinH3

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.

SecinH3 Chemical Structure

SecinH3 Chemical Structure

CAS: 853625-60-2

Selleck's SecinH3 has been cited by 4 Publications

2 Customer Reviews

Purity & Quality Control

Batch: S768501 DMSO] 92 mg/mL] false] Ethanol] 1 mg/mL] false] Water] Insoluble] false Purity: 99.62%
99.62

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Choose Selective cytohesin Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LOX cells Antiinvasive assay 30 uM Antiinvasive activity against human LOX cells assessed as inhibition of 5% FBS-induced cell invasion at 30 uM by Matrigel based cell invasion assay ChEMBL
Click to View More Cell Line Experimental Data

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] Click to View More Targets
2.4 μM 5.4 μM 5.4 μM 5.6 μM 5.6 μM
In vitro
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]
Kinase Assay 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 Research 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.
In Vivo
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]
Animal Research Animal Models Mice bearing H460 xenografts
Dosages 100 μL 2.5 mM, once daily
Administration i.p.

Chemical Information & Solubility

Molecular Weight 460.5 Formula

C24H20N4O4S

CAS No. 853625-60-2 SDF Download SecinH3 SDF
Smiles COC1=NN(C(=N1)C2=CC3=C(C=C2)OCO3)C4=CC=C(C=C4)NC(=O)CSC5=CC=CC=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (199.78 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

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.

Handling Instructions

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