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Product name : SGI-1027
Item : CR1950
Price : 100mg, $845; 500mg, $1785
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CAS : 1020149-73-8
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Details:
 

Chemical Information

M.Wt 461.52 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C27H23N7O
CAS No 1020149-73-8
Solubility

DMSO



Biological Activity of SGI-1027

 

SGI-1027 is a potent and selective inhibitor of DNA methyltransferase (DNMT) with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B, respectively.
IC50 value: 6/8/7.5 uM (DNMT1/3A/3B) [1]
Target: DNMT1/3A/3B
SGI-1027, inhibits the activity of DNMT1, DNMT3A, and DNMT3B as well M. SssI with comparable IC(50) (6-13 micromol/L) by competing with S-adenosylmethionine in the methylation reaction. Treatment of different cancer cell lines with SGI-1027 resulted in selective degradation of DNMT1 with minimal or no effects on DNMT3A and DNMT3B. At a concentration of 2.5 to 5 micromol/L (similar to that of decitabine), complete degradation of DNMT1 protein was achieved within 24 h without significantly affecting its mRNA level [1]. 

 

[1]. Datta J, et al. A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. Cancer Res. 2009 May 15;69(10):4277-85.


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