420204-M
Histone Lysine Demethylase Inhibitor VII, GSK-J1
别名:
Histone Lysine Demethylase Inhibitor VII, GSK-J1, JHDM Inhibitor II, 3-(6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoic acid
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关于此项目
经验公式（希尔记法）:
C22H23N5O2
化学文摘社编号:
分子量:
389.45
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.54
SMILES string
N3(CCc4c(cccc4)CC3)c1nc(nc(c1)NCCC(=O)O)c2ncccc2
InChI
1S/C22H23N5O2/c28-21(29)8-12-24-19-15-20(26-22(25-19)18-7-3-4-11-23-18)27-13-9-16-5-1-2-6-17(16)10-14-27/h1-7,11,15H,8-10,12-14H2,(H,28,29)(H,24,25,26)
InChI key
AVZCPICCWKMZDT-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
light yellow
solubility
DMSO: 100 mg/mL
Quality Level
General description
A pyridinyl-pyrimidinylaminopropanoic acid that effectively inhibits KDM6 family H3K27me3 demethylases JMJD3 (IC50 = 0.06 and 18 µM, respectively, by AlphaScreen and MALDI Mass detection method) and UTX (IC50 = 56 µM by MALDI Mass detection) in a α-ketoglutarate-competitive, peptide substrate-non-competitive manner, displaying much reduced potency against JARID1C, JMJD1a, JMJD2a, JMJD2c, JMJD2d, JMJD2e, 112 kinases, as well as a panel of 60 non-kinase enzymes, GPCRs, ion channels, nuclear receptors, and transporters. Recommended for cell-free assays only. For culture treatment, use the cell-permeable pro-drug GSK-J4 (Cat. No. 420205). Structural analysis reveals that the effective inhibition is a result of concerted action of GSK-J1 against the bindings of α-ketoglutarate, histone H3, as well as Fe+2 at the enzyme active site.
Biochem/physiol Actions
Primary Target
H3K27me3 demethylases JMJD3 & UTX
H3K27me3 demethylases JMJD3 & UTX
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Heinemann, B., et al. 2014. Nature514 E1.
Kruidenier, L., et al. 2014. Nature514, E2.
Kruidenier, L., et al. 2012. Nature488, 404.
Kruidenier, L., et al. 2014. Nature514, E2.
Kruidenier, L., et al. 2012. Nature488, 404.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
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