ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate
ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate Basic information
- Product Name:
- ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate
- Synonyms:
-
- 159142
- ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate
- KDM5 inhibitor C70
- KDOAM 21
- KDM5-C49,Histone Demethylase,JARID1,retinoblastoma,inhibit,KDM5 C70,KDM5-C70,KDM-5-C70,phosphorylation,KDM5C70,KDM5,Inhibitor,H3K4me3,antiproliferative
- 4-Pyridinecarboxylic acid, 2-[[[2-[[2-(dimethylamino)ethyl]ethylamino]-2-oxoethyl]amino]methyl]-, ethyl ester
- KDM5-C70(KDM5inhibitorC70)
- KDOAM-21 (KDM5-C70)
- CAS:
- 1596348-32-1
- MF:
- C17H28N4O3
- MW:
- 336.42922
- Mol File:
- 1596348-32-1.mol
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ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate Chemical Properties
- Boiling point:
- 466.6±45.0 °C(Predicted)
- Density
- 1.099±0.06 g/cm3(Predicted)
- storage temp.
- -10 to -25°C
- solubility
- Chloroform: soluble; DMSO: soluble; Ethanol: soluble
- pka
- 8.39±0.28(Predicted)
- form
- Liquid
- color
- Light yellow to yellow
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ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate Usage And Synthesis
Uses
KDOAM 21 is an inhibitor to KDM5A (Lysine Demethylase 5A) which is a protein coding gene.
Biological Activity
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).
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ethyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate(1596348-32-1)Related Product Information
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