GSK-J4

SKU: orb1697740

Description

GSK-J4

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1373423-53-0
• MW: 417.5
• Purity: 98.24%
• Formula: C₂₄H₂₇N₅O₂
• SMILES: CCOC(=O)CCNc1cc(nc(n1)-c1ccccn1)N1CCc2ccccc2CC1
• Target: Apoptosis,Histone Demethylase
• Solubility: DMSO:141 mg/mL (337.72 mM);Ethanol:41.75 mg/mL (100 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4.18 mg/mL (10.01 mM)

Bioactivity

• Target IC50:
  JMJD3:
• In Vivo:
  METHODS: To investigat the effect on sepsis, GSK-J4 (1-3 mg/kg) was administered intraperitoneally to ICR mice, and sepsis was induced by injection of bacterial suspension 1 h later. Results: Pharmacological Inhibition of JMJD3 by GSKJ4 protected mice from early septic death and reduce the production o the pro-inflammatory cytokine IL-1β an the expression of IL-6, TNF-α and MCP-1.
• In Vitro:
  METHODS: Prostate cancer cell lines R1-AD1, R1-D567, R1-I567, CWR22Rv-1 and PC3 were treated with GSK-J4 (0-32 µM) for 72 h. Cell viability was measured by Alamar blue reagent. Results: GSK-J4 had cell growth inhibitory and/or cytotoxic effects on PC cells. cWR22Rv-1 wa the most sensitive to the treatment, with an ED50 of about 3 µM METHODS: Human acute myeloid leukemia cells KG-1a were treated with GSK-J4 (2-10 µM) for 48 h. Apoptosis was detected by Flow cytometry. Results the apoptosis rate of KG-1a cells in the GSK-J4 treatment group was significantly increased compared wit the control group.
• Animal Research:
  GSK-J4 is prepared in DMSO and diluted 1/10 with ethanol.Six-to eight-week-old f Male C57BL/6 WT mice are injected by subcutaneous injection (s.c.) with 50 μg myelin oligodendrocyte glycoprotein 35-55 peptide (pMOG) emulsified in Complete Freund's Adjuvant (CFA) supplemented with heat-inactivated Mycobacterium tuberculosis H37 RA. In addition, mice receive intraperitoneal injection (i.p.) of 500 ng of pertussis toxin on days 0 and 2. Clinical signs are assessed daily according to the following scoring criteria: 0, no detectable signs; 1, flaccid tail; 2, hind limb weakness or abnormal gait; 3, complete hind limb paralysis; 4, paralysis of fore and hind limbs; and 5, moribund or death. A stock solution of GSK-J4 of 42 mg mL (100 mM) is prepared in dimethyl sulfoxide (DMSO) to preserve stability. Before injection the stock solution is diluted 1/10 with ethanol (DMSO: ethanol, 1:10 v/v) and brought to a final concentration of 140 μg mL in PBS. In systemic drug evaluation experiments, Each mouse receive daily i.p. injections (from days 0-5) of 100 μL of this solution containing 14.0 μg o the GSK-J4 (equivalent to 0.56 mg/kg o the drug). Control mice receive 100 μL o the Vehicle durin the same period. In Other EAE experiments, 106 bone marrow-derived DCs from WT mice are treated with GSK-J4 or Vehicle alone for 16 h, pulsed with 5 μg mL of pMOG for 4 h and then transferred i.v. into WT C57BL/6 recipient mice 14 and 7 days before EAE induction. In Other adoptive transfer EAE experiments, CD4+Foxp3+ Treg cells generated in the presence or absence of 25 nM GSK-J4 are purified by cell sorting and then 0.7 × 06 transferred i.v. into WT C57BL/6 recipient mice 1 day before EAE induction.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Apoptosis, demethylase, dendritic, H3K27me3/me2, GSK J4, GSK J4 HCl, GSKJ4, GSK-J-4, GSK-J4, HistoneDemethylase, Histone Demethylase, JMJD3, TGF-β, Th17, Th1

Compound Identifiers

PubChem CID

71729975