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Product Details

GSK-J4 | JMJ H3K27 Demethylase inhibitor (Cell Permeable)

GSK-J4 (1373423-53-0) is a histone demethylase JMJD3/UTX inhibitor. Inhibits demethylation of histone H3K27. Reduces LPS-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 μM for the inhibition of TNFα release). Cell permeable, ethyl ester of GSK J1 (cat.# 10-1393)1. GSK-J4 rescues newborn pups from embryonic lethality in BRAF knockin mice which recapitulate major features of RASopathies2.

References/Citations
1) Kruidenier et al. (2012), Selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response; Nature, 488 404
2) Inoue et al. (2014) New Braf knockin mice provide a pathogenic mechanism of developmental defects and therapeutic approach in cardio-facio-cutaneous syndrome; Hum. Mol. Genet., July 17, Epub ahead of print

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GSK-J4 | 1373423-53-0 | Structure | Supplier

Catalog#  10-1394

$75.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1373423-53-0
Catalog Number:
10-1394
Activity:
JMJ H3K27 Demethylase inhibitor (Cell Permeable)
Chemical Name:
N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine ethyl ester
Molecular Weight:
417.48
Molecular Formula:
C24H27N5O2
Solubility:
Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 40 mg/ml).
Physical Properties:
Yellow waxy solid
Purity:
99% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol 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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