853625-60-2 Usage
Description
N-[4-[5-(1,3-BENZODIOXOL-5-YL)-3-METHOXY-1H-1,2,4-TRIAZOL-1-YL]PHENYL]-2-(PHENYLTHIO)ACETAMIDE, also known as SecinH3, is a cell-permeable triazolo compound that functions as a Sec7 cytohesin inhibitor. It is characterized by its ability to selectively bind and antagonize the cytohesin family of small guanine nucleotide exchange factors (GEFs). N-[4-[5-(1,3-BENZODIOXOL-5-YL)-3-METHOXY-1H-1,2,4-TRIAZOL-1-YL]PHENYL]-2-(PHENYLTHIO)ACETAMIDE exhibits high affinity for the Sec7 domain, with a dissociation constant (Kd) of less than or equal to 250 nM for Sec7 from human cytohesins 1-3. It demonstrates inhibitory effects on large GEFs only at significantly higher concentrations and shows minimal activity against a panel of commonly studied kinases or hSosII.
Uses
Used in Pharmaceutical Industry:
N-[4-[5-(1,3-BENZODIOXOL-5-YL)-3-METHOXY-1H-1,2,4-TRIAZOL-1-YL]PHENYL]-2-(PHENYLTHIO)ACETAMIDE is used as a Sec7 domain-binding inhibitor for the development of pharmaceutical agents targeting cytohesin family small GEFs. Its high selectivity and potency make it a valuable tool in the study and potential treatment of diseases associated with the dysregulation of these proteins.
Used in Research Applications:
In the field of research, N-[4-[5-(1,3-BENZODIOXOL-5-YL)-3-METHOXY-1H-1,2,4-TRIAZOL-1-YL]PHENYL]-2-(PHENYLTHIO)ACETAMIDE serves as a valuable compound for investigating the role of cytohesin family small GEFs in various cellular processes. Its ability to effectively inhibit insulin signaling in both in vitro and in vivo models highlights its potential use in studying insulin-related pathways and their implications in metabolic disorders.
Used in Drug Discovery and Development:
N-[4-[5-(1,3-BENZODIOXOL-5-YL)-3-METHOXY-1H-1,2,4-TRIAZOL-1-YL]PHENYL]-2-(PHENYLTHIO)ACETAMIDE is utilized in drug discovery and development efforts to identify novel therapeutic agents that can modulate the activity of cytohesin family small GEFs. Its selectivity and potency make it an attractive starting point for the design and optimization of new drugs targeting these proteins for the treatment of various diseases.
Biological Activity
Sec7-specific GEF inhibitor that displays selectivity for small GEFs of the cytohesin family (IC 50 values are 2.4, 5.4, 5.4, 5.6, 5.6, 65 and > 100 μ M for hCyh2, hCyh1, mCyh3, hCyh3, drosophila steppke, yGea2-S7 and hEFA6-S7 respectively). Inhibits insulin signaling via inhibition of insulin receptor substrate protein (IRS) phosphorylation.
Biochem/physiol Actions
Primary TargetCytohesin
Check Digit Verification of cas no
The CAS Registry Mumber 853625-60-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,5,3,6,2 and 5 respectively; the second part has 2 digits, 6 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 853625-60:
(8*8)+(7*5)+(6*3)+(5*6)+(4*2)+(3*5)+(2*6)+(1*0)=182
182 % 10 = 2
So 853625-60-2 is a valid CAS Registry Number.
853625-60-2Relevant articles and documents
Affinity-based labeling of cytohesins with a bifunctional SecinH3 photoaffinity probe
Bi, Xihe,Schmitz, Anton,Hayallah, Alaa M.,Song, Jin-Na,Famulok, Michael
scheme or table, p. 9565 - 9568 (2009/05/06)
(Chemical Equation Presented) The specific binding of the cytohesin inhibitor SecinH3 to Sec7 domains of cytohesins was shown by the use of a bifunctional photoaffinity probe (see structure) on guanine nucleotide exchange factors (GEFs) and GTPases. This probe should be useful for the proteome-wide profiling of cytohesin complexes and the identification of the binding site.
