SGI-1027An inhibitor of the DNA methyltransferases

SGI-1027 (CAS 1020149-73-8)

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Synonym: N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide
Application: An inhibitor of the DNA methyltransferases
CAS Number: 1020149-73-8
Molecular Weight: 461.52
Molecular Formula: C27H23N7O
* Refer to Certificate of Analysis for lot specific data (including water content).
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SGI-1027 is an inhibitor of the DNA methyltransferases DNMT1, DNMT3A, and DNMT3B. It has been shown to cause the degradation of DNMT1 and to reactivate silenced tumor suppressor genes by reducing CpG island hypermethylation

Physical State :
Solid
Solubility :
Soluble in DMSO (92 mg/ml at 25 °C), DMF (~5 mg/ml), DMSO:PBS (pH 7.2)(1:4) (~0.2 mg/ml), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C).
Storage :
Store at -20° C
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.79 (Predicted)
IC50 :
Dnmt1: IC50 = 0.85 µM (human); Cytotoxicity against human U937 cells: IC50 = 1.7 µM; Dnmt3b: IC50 = 7.5 µM (murine); Dnmt3a: IC50 = 8 µM (murine); CpG DNA methylase M.SssI: IC50 = 13.5 µM (mycoplasma Spiroplasma sp. strain MQ1)
pK Values :
pKa: 9.82 (Predicted), pKb: 0.18 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
24858111
SMILES :
CC1=CC(=NC(=N1)N)NC2=CC=C(C=C2)NC(=O)C3=CC=C(C=C3)NC4=CC=NC5=CC=CC=C54

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Certificate of Analysis

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