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

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
Stability:
Stable for 2 years from date of purchase  as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

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

GSK-J1 | JMJ H3K27 Demethylase inhibitor (Non-cell permeable) is also available in the Cellular Metabolism Library.
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
Stability:
Stable for 2 years from date of purchase  as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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