GSK J4A cell permeable inhibitor of the histone demethylase JMJD3/UTX

GSK J4

GSK J4 is rated 5.0 out of 5 by 1.
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Synonym: Histone Lysine Demethylase Inhibitor VIII; GSK-J1 Pro-Drug; JMJD3 Inhibitor II
Application: A cell permeable inhibitor of the histone demethylase JMJD3/UTX
Purity: ≥98%
Molecular Weight: 417.50
Molecular Formula: C24H27N5O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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GSK J4 is a cell permeable prodrug rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases. The prodrug GSK-J4 inhibited TNF-α production with an IC50 of 9 μM in LPS-stimulated human macrophages and blocked the production of TNF-α by macrophages derived from patients with rheumatoid arthritis. GSK J4 is an inhibitor of JMJD3 and UTX.

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (100 mM).
Storage :
Store at 4° C
Boiling Point :
~581.2° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.62 (Predicted)
IC50 :
JMJD3: IC50 = 60 nM; TNFα release: IC50 = 9 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
71729975
MDL Number :
MFCD22683852
SMILES :
CCOC(=O)CCNC1=NC(=NC(=C1)N2CCC3=CC=CC=C3CC2)C4=CC=CC=N4

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Kamikawa et al Kamikawa et al. (PubMed ID 25993097) found that GSK-J4 inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells. -SCBT Publication Review
Date published: 2015-06-15
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