GSK J1( GSKJ1 | GSKJ 1 | GSKJ-1 )

Catalog No. M17982 CAS No. 1373422-53-7

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GSK J1
Note

Research use only, not for human use.
Brief Description

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.
Description

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.
In Vitro

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In Vivo

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Synonyms

GSKJ1 | GSKJ 1 | GSKJ-1
Pathway

Others
Target

Other Targets
Recptor

JMJD3 (KDM6B)|UTX (KDM6A)
Research Area

Others-Field
Indication

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CAS Number

1373422-53-7
Formula Weight

389.45
Molecular Formula

C22H23N5O2
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 33 mg/mL; 84.73 mM
SMILES

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

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