GSK-J1

GSK-J1, a chemical probe, is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.

Product Specifications

CAS Number

[1373422-53-7]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Histone Demethylase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GSK-J1.html

Purity

99.94

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

OC(CCNC1=NC(C2=NC=CC=C2)=NC(N(CC3)CCC4=C3C=CC=C4)=C1)=O

Molecular Formula

C22H23N5O2

Molecular Weight

389.45

Precautions

H315, H319, H335

References & Citations

[1]Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488 (7411) :404-8.|[2]Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514 (7520) :E1-2|[3]Horton JR, et al. Characterization of a Linked Jumonji Domain of the KDM5/JARID1 Family of Histone H3 Lysine 4 Demethylases. J Biol Chem. 2016 Feb 5;291 (6) :2631-46.