GSK J1

Research use only, not for human use.

GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively.

GSKJ1 is a selective and potent histone demethylase inhibitor (GSK-J1) that has significant activity (IC50 60 nM for human JmjD3) in vitro and in cells using an ester derivative (GSK-J4: 1 μM < IC50 < 10 μM; e.g. 9 μM in primary human macrophages). The pyridine regio-isomer GSK-J2 displays significantly less on-target activity (IC50 > 100 μM for human JmjD3) and thus can be used as control for target effects in vitro, and as ester derivative (GSK-J5) in cells. Recent data has shown that GSK-J1 also shows some activity (IC50 950 nM for Jarid1b, IC50 1.76 uM for Jarid1c) against H3K4me3/2/1 demethylases.

GSKJ1; GSKJ 1; GSKJ-1

Others

Other Targets

JMJD3 (KDM6B);UTX (KDM6A)

Others-Field

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1373422-53-7

389.45

C22H23N5O2

98%

DMSO : ≥ 33 mg/mL; 84.73 mM

OC(=O)CCNC1=CC(=NC(=N1)C1=CC=CC=N1)N1CCC2=C(CC1)C=CC=C2

3-((2-(pyridin-2-yl)-6-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)pyrimidin-4-yl)amino)propanoic acid

(-20℃)

With Ice Pack

≥ 2 years