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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
2 mg | $48 | In Stock | |
5 mg | $81 | In Stock | |
10 mg | $129 | In Stock | |
25 mg | $229 | In Stock | |
50 mg | $382 | In Stock | |
100 mg | $562 | In Stock | |
200 mg | $785 | In Stock | |
1 mL x 10 mM (in DMSO) | $142 | In Stock |
Description | GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro. |
Targets&IC50 | JMJD3 (cell-free assay):60 nM, JMJD3:50 μM |
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). |
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. |
Alias | GSK J4 HCl, GSK J4 HCl (1373423-53-0 free base) |
Molecular Weight | 453.97 |
Formula | C24H28ClN5O2 |
Cas No. | 1797983-09-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 20 mg/mL DMSO: 50 mg/mL (110.14 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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