GSK-J4 Hydrochloride

SKU: orb1302901

Description

GSK-J4 Hydrochloride

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1797983-09-5
• MW: 453.97
• Purity: 97.95% (May vary between batches)
• Formula: C₂₄H₂₈ClN₅O₂
• SMILES: Cl.CCOC(=O)CCNc1cc(nc(n1)-c1ccccn1)N1CCc2ccccc2CC1
• Target: Histone Demethylase
• Solubility: DMSO:50 mg/mL (110.14 mM);Ethanol:20 mg/mL (44.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.41 mM)

Bioactivity

• Target IC50:
  JMJD3 (cell-free assay):60 nM|JMJD3:50 μM
• In Vivo:
  Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.
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• In Vitro:
  When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 μM).
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

1373423-53-0, 1373423-53-0 free base, cells, diabetic, demethylase, dendritic, H3K27me3/me2, GSK J4 HCl, GSK J4 HCl (1373423-53-0 free base), GSK J4 Hydrochloride, GSK-J4, GSKJ4 Hydrochloride, GSK-J4 Hydrochloride, GSK-J-4 Hydrochloride, HistoneDemethylase, Histone Demethylase, Inhibitor, JMJD3, inhibit, inflammation, mice, TGF-β, Th1, Th17

Compound Identifiers

PubChem CID

71729974