SML3395
KDM5-C70
≥95% (HPLC)
别名:
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
质量水平
方案
≥95% (HPLC)
表单
oil
颜色
, Light yellow to very dark red-bown
储存温度
-10 to -25°C
SMILES字符串
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
InChI key
WCILOMUUNVPIKQ-UHFFFAOYSA-N
相关类别
生化/生理作用
Histone H3K4 demethylase inhibitor KDM5-C49 ethyl ester prodrug that selectively upregulates H3K4me3 and inhibits KDM5-dependent cancer growth.
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).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds
Cell Chemical Biology, 23(7), 769-781 (2016)
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
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
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 (
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