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KDM5-C49, JARID1 Histone Demethylases Inhibitor

KDM5-C49, JARID1 Histone Demethylases Inhibitor

$139.00
A potent and selective inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases
Catalog No. Unit Price Qty
M60191-2s 2mg solid $139.00
M60191-2 10 mM in DMSO (0.648 mL) $139.00

Details

Product Information
Molecular Weight: 308.38
Formula: C15H24N4O3
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: 4oC 1 year. DMSO: 4oC 3 month; -20oC 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-binding site. 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. 

KDM5-C49_spec.pdf

KDM5-C49_MSDS.pdf

 

Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 308.38
Formula: C15H24N4O3
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: 4oC 1 year. DMSO: 4oC 3 month; -20oC 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-binding site. 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. 

KDM5-C49_spec.pdf

KDM5-C49_MSDS.pdf

 

Products are for research use only. Not for human use.

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