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SGI-1027 DNMT inhibitor

Catalog No.B1622
Size Price Stock Qty
10mM (in 1mL DMSO)
$113.00
In stock
10mg
$103.00
In stock
100mg
$679.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

SGI-1027

Biological Activity

Description SGI-1027 is an inhibitor of DNMT with IC50 values of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B, respectively
Targets DNMT1 DNMT3B DNMT3A      
IC50 6 μM 7.5 μM 8 μM      

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Chemical Properties

Cas No. 1020149-73-8 SDF Download SDF
Chemical Name N-[4-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl]-4-(quinolin-4-ylamino)benzamide
Canonical SMILES CC1=CC(=NC(=N1)N)NC2=CC=C(C=C2)NC(=O)C3=CC=C(C=C3)NC4=CC=NC5=CC=CC=C54
Formula C27H23N7O M.Wt 461.52
Solubility >22.25mg/mL in DMSO Storage Store at -20° C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

SGI-1027 is an inhibitor of DNMT with IC50 values of 12.5μM, 8μM and 7.5μM, respectively for DNMT1, DNMT3A and DNMT3B [1].

SGI-1027 shows inhibition with mammalian DNMTs and bacterial M. SssI in vitro. Both the endogenous and recombinant DNMTs can be inhibited by SGI-1027. The mechanism of this inhibition is that SGI-1027 competes with Ado-Met but not the substrate DNA within the cofactor binding site of the enzyme. SGI-1027 inhibits DNA methylation through directly inhibiting DNMTs [1].

In cancer cells, many TSGs are silenced due to hypermethylation of CpG islands in their promoters. SGI-1027 can demethylates these CpG islands and reactivate the silenced TSGs. In RKO cells, prolonged treatment of SGI-1027 induces reexpression of P16 and TIMP3 genes. Moreover, SGI-1027 is found to cause selective degradation of DNMT1 via proteasomal pathway [1].

References:
[1] Datta J, Ghoshal K, Denny WA, Gamage SA, Brooke DG, Phiasivongsa P, Redkar S, Jacob ST. 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.