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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51142560
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 420204-10MG
- CAS:
- 1373422-53-7
