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<<Synonyms: GSK-J1 Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate, JHDM Inhibitor II Pro-Drug
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Overview
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Pricing & Availability
Catalog Number | Availability | Packaging | Qty/Pack | Price | Quantity | |
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420205-10MG |
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Glass bottle | 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, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate, JHDM Inhibitor II Pro-Drug |
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 |
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Packaged under inert gas | Packaged under inert gas |
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Specifications |
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Global Trade Item Number | |
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Catalog Number | GTIN |
420205-10MG | 04055977210798 |
Documentation
Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem SDS
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Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem Certificates of Analysis
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420205 |
References
Reference overview |
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Heinemann, B., et al. 2014. Nature 514 E1. Kruidenier, L., et al. 2014. Nature 514, E2. Kruidenier, L., et al. 2012. Nature 488, 404. |
Technical Info
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Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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