SGI 1027 - ≥98% (HPLC), high purity , CAS No.1020149-73-8, Inhibitor of DNA methyltransferase 1

Item Number
S288597
Grouped product items
SKUSizeAvailabilityPrice Qty
S288597-5mg
5mg
In stock
$83.90
S288597-10mg
10mg
In stock
$133.90
S288597-25mg
25mg
In stock
$301.90
S288597-50mg
50mg
In stock
$402.90
S288597-100mg
100mg
In stock
$725.90

DNA methyltransferase inhibitor

Basic Description

Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsDNA methyltransferase inhibitor. Inhibits the mammalian DNA methyltransferases DNMT3B, DNMT3A and DNMT1 (IC50values are 7.5, 8 and 12.5μM with Poly(dl-dC) as the substrate). Reactivates silenced tumor suppressor genes by reducing CpG island hypermethylati
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of DNA methyltransferase 1
Product Description

Application:

SGI-1027 has been used as a DNA methyltransferase inhibitor to study its effects on gene expression during osteogenic differentiation. It has also been used as a DNA methyltransferase 3a inhibitor to study its effects on interleukin-6 (IL-6)-induced loss of forkhead box P3 (Foxp3) gene expression in B-lymphocyte-induced maturation protein 1 (Blimp1)-Treg cells.


Associated Targets(Human)

DNMT3A Tclin DNA (cytosine-5)-methyltransferase 3A (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DNMT1 Tclin DNA (cytosine-5)-methyltransferase 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
DNMT1 Tclin DNA (cytosine-5)-methyltransferase 1 (978 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DNMT3A Tclin DNA (cytosine-5)-methyltransferase 3A (310 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP2K3 Tchem Dual specificity mitogen-activated protein kinase kinase 3 (632 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AOX1 Tchem Aldehyde oxidase (429 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
K562 (73714 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PC-3 (62116 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Raji (5516 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U-937 (7138 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCT-116 (91556 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2 (196354 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KG-1 (867 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDA-MB-231 (73002 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PBMC (10003 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DNMT3B Tchem DNA (cytosine-5)-methyltransferase 3B (150 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EHMT1 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 (407 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EHMT2 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (93046 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DNMT3A Tclin DNMT3A2/3L complex (48 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MYC Tchem c-Myc/c-Max (51 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Prmt1 Protein arginine N-methyltransferase 1 (55 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences
DNA (cytosine-5)-methyltransferase 1 inhibitorINHIBITORALA1993DNA (cytosine-5)-methyltransferase 1SINGLE PROTEINHomo sapiens

DailyMed: [1]


Wikipedia: [1] , [2]


DNA (cytosine-5)-methyltransferase 1 inhibitorINHIBITORALA1993DNA (cytosine-5)-methyltransferase 1SINGLE PROTEINHomo sapiens

DailyMed: [1]


Wikipedia: [1]


DNA (cytosine-5)-methyltransferase 3A inhibitorINHIBITORALA1992DNA (cytosine-5)-methyltransferase 3ASINGLE PROTEINHomo sapiens

DailyMed: [1]


Wikipedia: [1] , [2]


DNA (cytosine-5)-methyltransferase 3A inhibitorINHIBITORALA1992DNA (cytosine-5)-methyltransferase 3ASINGLE PROTEINHomo sapiens

DailyMed: [1]


Wikipedia: [1]


Names and Identifiers

Pubchem Sid504769881
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/504769881
IUPAC Name N-[4-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl]-4-(quinolin-4-ylamino)benzamide
INCHI InChI=1S/C27H23N7O/c1-17-16-25(34-27(28)30-17)32-20-10-12-21(13-11-20)33-26(35)18-6-8-19(9-7-18)31-24-14-15-29-23-5-3-2-4-22(23)24/h2-16H,1H3,(H,29,31)(H,33,35)(H3,28,30,32,34)
InChi Key QSYLKMKIVWJAAK-UHFFFAOYSA-N
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
Isomeric SMILES CC1=CC(=NC(=N1)N)NC2=CC=C(C=C2)NC(=O)C3=CC=C(C=C3)NC4=CC=NC5=CC=CC=C54
PubChem CID 24858111
Molecular Weight 461.52

Certificates

C of A & Other Certificates(BSE/TSE, COO)

Find and download the COA for your product by matching the lot number on the packaging.

5 results found

Lot NumberCertificate TypeDateItem
I2227633Certificate of AnalysisAug 17, 2022 S288597
I2227635Certificate of AnalysisAug 17, 2022 S288597
I2227636Certificate of AnalysisAug 17, 2022 S288597
I2227637Certificate of AnalysisAug 17, 2022 S288597
I2227647Certificate of AnalysisAug 17, 2022 S288597

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 23.08, Max Conc. mM: 50

Related Documents

References

1. Valente S, Liu Y, Schnekenburger M, Zwergel C, Cosconati S, Gros C, Tardugno M, Labella D, Florean C, Minden S et al..  (2014)  Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells..  J Med Chem,  57  (3): (701-13).  [PMID:24387159] [10.1021/op500134e]

Solution Calculators