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420205 Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem

Overview

Replacement Information

Products

Catalogue NumberPackaging Qty/Pack
420205-10MGCN Glass bottle 10 mg
Description
OverviewA 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 Number420205
Brand Family Calbiochem®
SynonymsGSK-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
ReferencesHeinemann, 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
CAS number1373423-53-0
FormTan semi-solid
Hill FormulaC₂₄H₂₇N₅O₂
Chemical formulaC₂₄H₂₇N₅O₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationHistone 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).
Biological Information
Primary TargetH3K27me3 demethylases JMJD3 & UTX
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months for -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
420205-10MGCN 04055977210798

Documentation

Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem Certificates of Analysis

TitleLot Number
420205

References

Reference overview
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

Title
White Paper - The Message in the Marks: Deciphering Cancer Epigenetics
Data Sheet

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.

Revision06-September-2013 JSW
SynonymsGSK-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
DescriptionThe H3K27me3 demethylase inhibitor GSK-J1 (Cat. No. 420204) 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.
FormTan semi-solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1373423-53-0
Chemical formulaC₂₄H₂₇N₅O₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months for -20°C.
Toxicity Standard Handling
ReferencesHeinemann, B., et al. 2014. Nature 514 E1.
Kruidenier, L., et al. 2014. Nature 514, E2.
Kruidenier, L., et al. 2012. Nature 488, 404.