TargetMol

GSK-J4

Product Code:
 
TAR-T3100
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T3100-2mg2mg£111.00
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TAR-T3100-5mg5mg£137.00
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TAR-T3100-10mg10mg£176.00
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TAR-T3100-1mL1 mL * 10 mM (in DMSO)£186.00
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TAR-T3100-25mg25mg£262.00
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TAR-T3100-50mg50mg£379.00
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TAR-T3100-100mg100mg£538.00
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TAR-T3100-200mg200mg£662.00
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Further Information

Bioactivity:
GSK-J4 is a potent H3K27me3 demethylase inhibitor, with IC50s of 8.6 μM and 6.6 μM towards KDM6B and KDM6A respectively. It is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.
CAS:
1373423-53-0
Formula:
C24H27N5O2
Molecular Weight:
417.513
Pathway:
Apoptosis; Chromatin/Epigenetic
Purity:
0.9998
SMILES:
CCOC(=O)CCNc1cc(nc(n1)-c1ccccn1)N1CCc2ccccc2CC1
Target:
Apoptosis; Histone Demethylase

References

1. Kruidenier L, et al. Nature, 2012, 488(7411), 404-408. 2. Donas C, et al. The histone demethylase inhibitor GSK-J4 limits inflammation through the induction of a tolerogenic phenotype on DCs. J Autoimmun. 2016 Dec;75:105-117. 3. Lin B, Lu B, Hsieh I, et al. Synergy of GSK-J4 With Doxorubicin in KRAS-Mutant Anaplastic Thyroid Cancer[J]. Frontiers in Pharmacology. 2020, 11. 4. Chen, Hong, et al.? . Histone demethylase UTX is a therapeutic target for diabetic kidney disease [J]. J Physiol. 2019 Mar;597(6):1643-1660.