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SML3395

Sigma-Aldrich

KDM5-C70

≥95% (HPLC)

Synonyme(s) :

C 70, C-70, C70, Ethyl 2-(((2-((2-(dimethylamino)ethyl)ethylamino)-2-oxoethyl)amino)methyl)-4-pyridinecarboxylate, Ethyl 2-(((2-((2-(dimethylamino)ethyl)ethylamino)-2-oxoethyl)amino)methyl)isonicotinate, KDM5-C49 ethyl ester, KDOAM-20 ethyl ester, KDOAM-21, KDOAM20 ethyl ester, KDOAM21

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About This Item

Formule empirique (notation de Hill):
C17H28N4O3
Numéro CAS:
1596348-32-1
Poids moléculaire :
336.43
Numéro MDL:
MFCD30721931
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Essai

≥95% (HPLC)

Forme

oil

Couleur

, Light yellow to very dark red-bown

Température de stockage

-10 to -25°C

Chaîne SMILES 

CN(CCN(C(CNCC1=CC(C(OCC)=O)=CC=N1)=O)CC)C

InChI

1S/C17H28N4O3/c1-5-21(10-9-20(3)4)16(22)13-18-12-15-11-14(7-8-19-15)17(23)24-6-2/h7-8,11,18H,5-6,9-10,12-13H2,1-4H3

Clé InChI

WCILOMUUNVPIKQ-UHFFFAOYSA-N

Actions biochimiques/physiologiques

KDM5-C70 (KDOAM-21) corresponds to the ethyl ester precursor of a selective αKG-competitive KDM5 histone demethylase inhibitor KDM5-C49 (KDOAM-21; KDM5A/B/C/D Ki = 2/1/6.1/3.4 nM vs. KDM4C/6B/3A/2A Ki = 0.51/4.55/2.59/4.4 μM; KDM5A/B/C/D IC50 = 1.1/0.8/3.2/2.7 μM by FDH assay with [αKG] = 1 mM & [E]/[S] = 0.5/15 μM; KDM5A/B/C IC50 = 25/30/59 nM by alphaLISA with [αKG] = 25 μM & [E]/[S] = 10/100 nM). KDM5-C70 treatment selectively upregulates cellular histone H3 trimethylation on Lys4 (H3K4me3), but not on Lys9/7/36 (5 μM, 3d), and inhibits KDM5-dependent cancer growth (by 85%/MCF7/11d, 97%/BT474/24d, and 70%/ZR-75-1/24d; 5 μM).

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number
0000200182
0000211081
0000211080

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Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

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Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds
Cell Chemical Biology, 23(7), 769-781 (2016)
Lauren P Blair et al.
Science advances, 2(11), e1501662-e1501662 (2017-02-01)
The complexity by which cells regulate gene and protein expression is multifaceted and intricate. Regulation of 3' untranslated region (UTR) processing of mRNA has been shown to play a critical role in development and disease. However, the process by which
Stephanie B Hatch et al.
Epigenetics & chromatin, 10, 9-9 (2017-03-08)
Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and their tight associations with diseases including cancer and mental disorders. The first KDM inhibitors for KDM1 have entered clinical trials, and
Brian B Liau et al.
Cell stem cell, 20(2), 233-246 (2016-12-19)
Glioblastoma, the most common and aggressive malignant brain tumor, is propagated by stem-like cancer cells refractory to existing therapies. Understanding the molecular mechanisms that control glioblastoma stem cell (GSC) proliferation and drug resistance may reveal opportunities for therapeutic interventions. Here
John R Horton et al.
Journal of medicinal chemistry, 61(7), 3193-3208 (2018-03-15)
Isomers of chiral drugs can exhibit marked differences in biological activities. We studied the binding and inhibitory activities of 12 compounds against KDM5A. Among them are two pairs of enantiomers representing two distinct inhibitor chemotypes, namely, ( R)- and (
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