1527503-11-2 Usage
Uses
Used in Pharmaceutical Industry:
5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine is used as a potent peptide-competitive inhibitor for the lysine methyltransferase G9a. It exhibits a high degree of selectivity (1000 fold) over other methyl transferases, making it a valuable compound for the development of targeted therapies in the treatment of various diseases.
Used in Epigenetic Research:
In the field of epigenetics, 5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine is utilized as a research tool to study the role of G9a in gene regulation and its implications in disease pathology. By inhibiting G9a, researchers can gain insights into the epigenetic mechanisms that underlie various biological processes and disorders.
Used in Drug Development:
5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine serves as a lead compound in the development of new drugs targeting G9a-mediated processes. Its high selectivity and potency make it an attractive candidate for further optimization and refinement to create more effective and safer therapeutic agents.
Biochem/physiol Actions
A-366 is an SGC chemical probe for G9a/GLP, developed in collaboration with Abbvie. A-366 is a potent, selective inhibitor of the histone methyltransferase G9a. The IC50 values for G9a inhbition in enzymatic and cell based assays are 3.3 and approximately 3 μM, respectively. A-366 has little or no detectable activity against a panel of 21 other methyltransferases. For full characterization details, please visit the A-366 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
Check Digit Verification of cas no
The CAS Registry Mumber 1527503-11-2 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,5,2,7,5,0 and 3 respectively; the second part has 2 digits, 1 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1527503-11:
(9*1)+(8*5)+(7*2)+(6*7)+(5*5)+(4*0)+(3*3)+(2*1)+(1*1)=142
142 % 10 = 2
So 1527503-11-2 is a valid CAS Registry Number.
1527503-11-2Relevant academic research and scientific papers
INHIBITORS OF HISTONE METHYLTRANSFERASE G9a
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Paragraph 0208, (2015/12/23)
Described herein are compounds, pharmaceutical compositions and methods for treating cancer, inflammation, or autoimmune disease in a subject, or for inhibiting histone methyltransferase G9a.
Discovery and development of potent and selective inhibitors of histone methyltransferase G9a
Sweis, Ramzi F.,Pliushchev, Marina,Brown, Peter J.,Guo, Jun,Li, Fengling,Maag, David,Petros, Andrew M.,Soni, Nirupama B.,Tse, Chris,Vedadi, Masoud,Michaelides, Michael R.,Chiang, Gary G.,Pappano, William N.
supporting information, p. 205 - 209 (2014/03/21)
G9a is a histone lysine methyltransferase responsible for the methylation of histone H3 lysine 9. The discovery of A-366 arose from a unique diversity screening hit, which was optimized by incorporation of a propyl-pyrrolidine subunit to occupy the enzyme
