Home / Histone Demethylase Inhibitors / GSK J1

GSK J1

Catalog #: 4593
5 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4593/10
4593/50
GSK J1 | CAS No. 1373422-53-7 | Histone Demethylase Inhibitors
1 Image
Description: Potent JMJD3/UTX inhibitor

Chemical Name: N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine

Purity: ≥99%

Product Details
Citations (5)
Supplemental Products
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

GSK J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 (KDM6B) and UTX (KDM6A) (IC50 values are 28 and 53 nM respectively). Also inhibits KDM5B, KDM5C and KDM5A (IC50 values are 170, 550 and 6,800 nM respectively). Exhibits no activity against a panel of other histone demethylases (IC50 >20 μM), and displays no significant inhibitory activity against 100 protein kinases at a concentration of 30 μM.

Ethyl ester derivative and Negative Control also available.

Technical Data

M.Wt:
389.45
Formula:
C22H23N5O2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥99%
Storage:
Desiccate at RT
CAS No:
1373422-53-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the GSK J1 probe summary on the SGC website.
Other Product-Specific Information:

Background References

  1. Signalling couples hair follicle stem cell quiescence with reduced histone H3 K4/K9/K27me3 for proper tissue homeostasis
    J Lee, S Kang, KC Lilja, KJ Colletier, CJ Scheitz, YV Zhang, T Tumbar
    Nat Commun, 2016;7(0):11278.
  2. Inhibition of demethylases by GSK-J1/J4.
    Heinemann et al.
    Nature, 2014;514:E1
  3. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.
    Kruidenier et al.
    Nature, 2012;488:404

Product Datasheets

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Citations for GSK J1

The citations listed below are publications that use Tocris products. Selected citations for GSK J1 include:

5 Citations: Showing 1 - 5

  1. KDM6B promotes activation of the oncogenic CDK4/6-pRB-E2F pathway by maintaining enhancer activity in MYCN-amplified neuroblastoma.
    Authors: Jie Et al.
    Nat Commun  2021;12:7204
  2. Histone H3 K4/9/27 Trimethylation Levels Affect Wound Healing and Stem Cell Dynamics in Adult Skin.
    Authors: Aiko Et al.
    Stem Cell Reports  2020;14:34-48
  3. Targeting the H3K4 Demethylase KDM5B Reprograms the Metabolome and Phenotype of Melanoma Cells.
    Authors: Dirk Et al.
    J Invest Dermatol  2019;139:2506-2516.e10
  4. Signalling couples hair follicle stem cell quiescence with reduced histone H3 K4/K9/K27me3 for proper tissue homeostasis.
    Authors: Lee Et al.
    Cancer Metab  2016;7:11278
  5. Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism.
    Authors: Aspuria Et al.
    Nat Commun  2015;2:21

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