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SML3395

Sigma-Aldrich

KDM5-C70

≥95% (HPLC)

Synonyma:

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

Empirický vzorec (Hillův zápis):
C17H28N4O3
Číslo CAS:
1596348-32-1
Molekulová hmotnost:
336.43
MDL number:
MFCD30721931
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥95% (HPLC)

form

oil

color

, Light yellow to very dark red-bown

storage temp.

-10 to -25°C

SMILES string

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

Biochem/physiol Actions

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).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Osvědčení o analýze (COA)

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Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds
Cell Chemical Biology, 23(7), 769-781 (2016)
Catrine Johansson et al.
Nature chemical biology, 12(7), 539-545 (2016-05-24)
Members of the KDM5 (also known as JARID1) family are 2-oxoglutarate- and Fe(2+)-dependent oxygenases that act as histone H3K4 demethylases, thereby regulating cell proliferation and stem cell self-renewal and differentiation. Here we report crystal structures of the catalytic core of
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 (
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
Peter van Galen et al.
Molecular cell, 61(1), 170-180 (2015-12-22)
Genome-wide profiling of histone modifications can provide systematic insight into the regulatory elements and programs engaged in a given cell type. However, conventional chromatin immunoprecipitation and sequencing (ChIP-seq) does not capture quantitative information on histone modification levels, requires large amounts
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