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Xcessbio
KDM5-C49,JARID1HistoneDemethylasesInhibitor
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产品名称:
KDM5-C49,JARID1HistoneDemethylasesInhibitor
产品型号:
M60191-2s
产品展商:
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产品文档:
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简单介绍
KDM5-C49,JARID1HistoneDemethylasesInhibitor
KDM5-C49,JARID1HistoneDemethylasesInhibitor
的详细介绍
Product Information
Molecular Weight:
308.38
Formula:
C
15
H
24
N
4
O
3
Purity:
≥98%
CAS#:
n/a
Solubility:
DMSO up to 100 mM
Chemical Name:
2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinic acid
Storage:
Powder: 4
o
C 1 year. DMSO: 4
o
C 3 month; -20
o
C 1 year.
Biological Activity:
KDM5-C49 is a potent and selective inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases. It has IC50 ~40 nM, 160 nM and 100 nM for KDM5A, KDM5B and KDM5C respectively. It has >100-fold selectivity over KDM4 and KDM6 etc. KDM5-C49 occupies the aKG-. The highly polar carboxylate group of KDM5-C49 restricts its cellular permeability, so it has IC50 >1 µM for inhibiting demthylation of H3K4 in U2OS human osteosarcoma cell line and in human breast adenocarcinoma MCF7 tumor cell proliferation assay. Therefore KDM5-C70 was developed as a pro-drug, masking the polarity of the acid group of the KDM5-C49, for cellular assays and in vivo use.
How to Use:
In vitro:
KDM5-C49 was used at 1-10 µM in vitro.
In vivo:
n/a
Reference:
1. Marc Labelle, et al. Inhibitors of Histone Demethylases. (2014). PCT WO 2014053491
2. Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. (2016) Nat Chem Biol. 12(7):539-45.
3. Horton JR, et al. Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds. (2016) Cell Chem Biol. 23(7):769-81.
Products are for research use only. Not for human use.
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