Cat. No. Name Size Price Add Cart
KI2435GSK-J11 mg$156
GSK-J15 mg$234
GSK-J110 mg$390
GSK-J150 mg$1430
GSK-J1100 mg$2470

Chemical Characteristic

Product NameGSK-J1
SynonymsN/A
CAS No.1373422-53-7
Molecular Weight 389.45
FormulaC22H23N5O2
Chemical NameN-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-?-alanine
SmilesC(=O)(CCNc1nc(nc(c1)N1CCc2c(CC1)cccc2)c1ccccn1)O

Biological activities

GSK-J1 is a selective jumonji (JMJ) H3K27 demethylase inhibitor. GSK-J1 has an IC50 of 60 nM in the JMJD3 Alpha Screen assay. GSK-J1 is competitive with α-ketoglutarate but non-competitive with the histone peptide substrate. GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner.[1]

References

[1] Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012, 488(7411): 404-408.

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