SecinH3

SKU: orb1223028

Description

SecinH3 is a cytohesin antagonist.

Key Properties

• CAS Number: 853625-60-2
• MW: 460.5
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₀N₄O₄S
• SMILES: O=C(CSc1ccccc1)Nc1ccc(cc1)n1nc(OC)nc1c1ccc2OCOc2c1
• Target: Syk
• Solubility: DMSO : 100 mg/mL. 217.15 mM

Bioactivity

• In Vivo:
  compared with 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SecinH3 | Secin-H3 | Secin H3

Quick Database Links

Gene Symbol

Syk