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GSK-J1 | JMJ H3K27 Demethylase inhibitor (Non-cell permeable)

GSK-J1 (1373422-53-7) is a potent and selective inhibitor of jumonji H3K27 histone demethylases JMJD3 and UTX (IC50 = 60 nM, human JMJD3). This is the first known inhibitor selective for the H3K27me3-specific JMJ subfamily which binds to the active catalytic site of the enzyme. The COOH group confers cell impermeability and as such GSK-J1 is useful as a standard in in vitro assays. A cell permeable ethyl ester analog is also available, see GSK-J4 (cat.# 10-1394).

References/Citations
1) Kruidenier et al. (2012), A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response; Nature, 488 404

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Focus Biomolecules supplier, structure of GSK-J1 | JMJ H3K27 Demethylase inhibitor (Non-cell permeable) | CAS 1373422-53-7

Catalog#  10-1393

$75.00
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CAS:
1373422-53-7
Catalog Number:
10-1393
Activity:
JMJ H3K27 Demethylase inhibitor (Non-cell permeable)
Chemical Name:
N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine
Molecular Weight:
389.46
Molecular Formula:
C22H23N5O2
Solubility:
Soluble in DMSO (up to 20 mg/ml).
Physical Properties:
Pale yellow solid
Purity:
99% by TLC
NMR (Conforms)
Storage Temperature:
RT (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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