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SecinH3 

Cat. No.: HY-100559 Purity: 99.60%
Handling Instructions

SecinH3 is an antagonist of cytohesins with IC50s of 5.4 μM, 2.4 μM, 5.4 μM, 5.6 μM, 5.6 μM and 65 μM for hCyh1, hCyh2, mCyh3, hCyh3, drosophila steppke and yGea2-S7, respectively.

For research use only. We do not sell to patients.

SecinH3 Chemical Structure

SecinH3 Chemical Structure

CAS No. : 853625-60-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
25 mg USD 384 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1056 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SecinH3 is an antagonist of cytohesins with IC50s of 5.4 μM, 2.4 μM, 5.4 μM, 5.6 μM, 5.6 μM and 65 μM for hCyh1, hCyh2, mCyh3, hCyh3, drosophila steppke and yGea2-S7, respectively.

IC50 & Target

IC50: 5.4 μM (hCyh1),2.4 μM (hCyh2),5.4 μM (mCyh3),5.6 μM (hCyh3),5.6 μM (drosophila steppke), 65 μM (yGea2-S7)[1]

In Vitro

SecinH3 is a Sec7-specific guanine nucleotide exchange factor (GEF) inhibitor with preference for the small GEFs of the cytohesin family. SecinH3 almost completely blocks the insulin-dependent transcriptional repression of IGFBP1 with an IC50 of 2.2 μM. Insulin-stimulated translocation of ARF6 to the plasma membrane is also inhibited by SecinH3. It is found that SecinH3 inhibits the insulin-dependent phosphorylation of Akt and FoxO1A in a concentration-dependent manner. Insulin-induced exclusion of FoxO1A from the nucleus is completely prevented by SecinH3. The binding of IRS1 to the insulin receptor is also inhibited by SecinH3[1].

In Vivo

Compare to mice fed the same chow without SecinH3, the expression levels of the insulin-repressed gluconeogenic genes are elevated, whereas the insulin-induced glycolytic genes are reduced in SecinH3-treated mice. Insulin-stimulated Akt phosphorylation is also inhibited in SecinH3-treated mice. The expression of the genes for two key enzymes of mitochondrial β-oxidation, carnitine palmitoyltransferase 1a (Cpt1a) and hydroxyacyl-CoA dehydrogenase (Hadha), both of which are repressed by insulin, is increased in the SecinH3-treated mice. It is found significantly increased levels of serum insulin with slightly elevated glucose concentrations in SecinH3-treated mice. Accordingly, 3-hydoxybutyrate is increased in the serum of SecinH3-treated mice[1].

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (217.15 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1715 mL 10.8575 mL 21.7151 mL
5 mM 0.4343 mL 2.1715 mL 4.3430 mL
10 mM 0.2172 mL 1.0858 mL 2.1715 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

105 HepG2 cells are seeded in 12 well plates and cultured for 24 h in EMEM containing 10 % FCS. Cells are then serum starved in EMEM for 24 h and stimulated for 12 h with 10 nM insulin in the presence of SecinH3, the negative control D5 or vehicle (0.2% final concentration of DMSO). Total mRNA is prepared using Kit and cDNA for qPCR is generated from 1 μg RNA. qPCR is performed and data are normalized to β2-microglobulin expression[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

C57/Bl6N mice are kept on a 12 h light/dark cycle in a pathogen-free animal facility and fed ad libitum with standard mice diet. After feeding with standard diet or with the same diet containing 0.9 μmol/g SecinH3 for 3 days, mice are intraperitoneally injected with 100 μL saline containing or not 40 μg recombinant human insulin. After 10 min the mice are anaesthetized and the liver is removed and lysed in lysis buffer. Normalized amounts of protein are either separated by SDS-PAGE and transferred onto nitrocellulose, or immunoprecipitated using agarose-conjugated antibodies against IRβ or IRS1[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

460.51

Formula

C₂₄H₂₀N₄O₄S

CAS No.

853625-60-2

SMILES

O=C(NC1=CC=C(N2N=C(OC)N=C2C3=CC=C(OCO4)C4=C3)C=C1)CSC5=CC=CC=C5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SecinH3
Cat. No.:
HY-100559
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SecinH3

Cat. No.: HY-100559