420205 Sigma-AldrichHistone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem
Histone Lysine Demethylase Inhibitor VIII, GSK-J4, CAS 1373423-53-0, is converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (~ 25 to 50 µM in HeLa cultures).
More>> Histone Lysine Demethylase Inhibitor VIII, GSK-J4, CAS 1373423-53-0, is converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (~ 25 to 50 µM in HeLa cultures). Less<<Synonyme: GSK-J1 Pro-Drug, JHDM Inhibitor II Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate
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Preis & Verfügbarkeit
Bestellnummer | Verfügbarkeit | Verpackung | St./Pkg. | Preis | Menge | |
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420205-10MG |
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Glasflasche | 10 mg |
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Description | |
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Overview | A cell-permeable GSK-J1 (Cat. No. 420204) 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). |
Catalogue Number | 420205 |
Brand Family | Calbiochem® |
Synonyms | GSK-J1 Pro-Drug, JHDM Inhibitor II Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate |
References | |
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References | Heinemann, B., et al. 2014. Nature 514 E1. Kruidenier, L., et al. 2014. Nature 514, E2. Kruidenier, L., et al. 2012. Nature 488, 404. |
Product Information | |
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CAS number | 1373423-53-0 |
Form | Tan semi-solid |
Hill Formula | C₂₄H₂₇N₅O₂ |
Chemical formula | C₂₄H₂₇N₅O₂ |
Reversible | Y |
Structure formula Image | |
Quality Level | MQ100 |
Biological Information | |
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Primary Target | H3K27me3 demethylases JMJD3 & UTX |
Purity | ≥98% by HPLC |
Physicochemical Information | |
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Cell permeable | Y |
Packaging Information | |
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Packaged under inert gas | Packaged under inert gas |
Global Trade Item Number | |
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Bestellnummer | GTIN |
420205-10MG | 04055977210798 |