GSK-J1

SKU: orb1300411

Description

GSK-J1 is a potent and selective cell-permeable inhibitor of the H3K27me3/2 demethylases JMJD3 (KDM6B) and UTX (KDM6A), with IC50 values of 28 nM and 53 nM, respectively. It is widely used in vitro and in vivo to investigate the role of these enzymes in cancer, immunology, and stem cell biology.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1373422-53-7
• MW: 389.45
• Purity: 99.67% (May vary between batches)
• Formula: C₂₂H₂₃N₅O₂
• SMILES: OC(=O)CCNc1cc(nc(n1)-c1ccccn1)N1CCc2ccccc2CC1
• Target: Histone Demethylase
• Solubility: DMSO:38.9 mg/mL (99.88 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.14 mM);Ethanol:38.9 mg/mL (99.88 mM)

Bioactivity

• Target IC50:
  UTX (KDM6A):53 nM|JMJD3 (KDM6B):28 nM
• In Vitro:
  In HEK-293 cells, GSK-J1 inhibits the activities of transiently transfected JMJD3 and UTX. GSK-J1 also inhibits TNF-α production by human primary macrophages by increasing total nuclear H3K27me3 levels. In MC3T3-E1 cells, GSK-J1 suppresses Runx2 and Osterix expressions and ALP activity, and increases the global levels of H3K27me3.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSKJ1, GSK-J1, GSK-J-1, GSK J1, Histone Demethylase, HistoneDemethylase, Inhibitor, inhibit, JMJD3 (KDM6B), UTX (KDM6A)

Compound Identifiers

PubChem CID

56963315