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General description
A cell-permeable GSK-J1 prodrug that is ineffective in cell-free assays, but is effectively converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (effective conc. 25 to 50 µM in HeLa cultures). GSK-J4 treatment is shown to block LPS-induced TNF-α production in primary human macrophage cultures (IC50 = 9 µM by ELISA).
This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the SGC website (http://www.thesgc.org/scientists/chemical_probes/GSKJ1).
The H3K27me3 demethylase inhibitor GSK-J1 against JMJD3 and UTX is made cell-permeable by ethyl ester derivatization to facilitate cellular delivery ([medium GSK-J4]t=0 = 30 µM; [cellular GSK-J1]t=1h = 1.6 µM). The pro-drug GSK-J4, being ineffective in cell-free assays, is effectively converted to GSK-J1 intracellularly and inhibits nuclear H3K27me3 levels in both untransfected and JMJD3-transfected HeLa cells (25 to 50 µM). Simultaneous inhibition of cellular JMJD3 and UTX by GSK-J4 treatment is shown to block LPS-induced production of several proinflammatory cytokines, including TNF-α (IC50 = 9 µM by ELISA), in primary human macrophage cultures.
Biochem/physiol Actions
Cell permeable: yes
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months for -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | semisolid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | tan |
| solubility | DMSO: 100 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | N3(CCc4c(cccc4)CC3)c1nc(nc(c1)NCCC(=O)OCC)c2ncccc2 |
| InChI | 1S/C24H27N5O2/c1-2-31-23(30)10-14-26-21-17-22(28-24(27-21)20-9-5-6-13-25-20)29-15-11-18-7-3-4-8-19(18)12-16-29/h3-9,13,17H,2,10-12,14-16H2,1H3,(H,26,27,28) |
| InChI key | WBKCKEHGXNWYMO-UHFFFAOYSA-N |
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¥ 2622.09
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¥ 1563.36
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¥ 3372.68
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¥ 2883.61
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¥ 10277.12
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¥ 2666.57
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¥ 3404.94
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¥ 70526.15
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¥ 29754.56
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¥ 65710.50
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