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Histone Lysine Demethylase Inhibitor VII, GSK-J1 - CAS 1373422-53-7 - Calbiochem

Synonym: Histone Lysine Demethylase Inhibitor VII, GSK-J1 - CAS 1373422-53-7 - Calbiochem, JHDM Inhibitor II, 3-(6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoic acid

  • CAS Number 1373422-53-7

  • Empirical Formula (Hill Notation) C22H23N5O2

  • Molecular Weight 389.45

  •  MDL number MFCD22683851

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Properties

assay   ≥98% (HPLC)
form   powder
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   light yellow
solubility   DMSO: 100 mg/mL

Description

General description

A pyridinyl-pyrimidinylaminopropanoic acid that effectively inhibits KDM6 family H3K27m3 demethylases JMJD3 and UTX (IC50 = 18 and 56 µM, respectively, by MALDI Mass detection) in an α-ketoglutarate-competitive, peptide substrate-non-competitive manner, displaying much reduced potency against JARID1C, JMJD1a, JMJD2a, JMJD2c, JMJD2d, JMJD2e, as well as112 kinases and 60 non-kinase enzymes. Recommended for cell-free assays only. For culture treatment, use the cell-permeable pro-drug GSK-J4 (Cat. No. 420205).

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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