GSK-J4 - ≥98%, high purity , CAS No.1373423-53-0, Inhibitor of lysine demethylase 5B;Inhibitor of lysine demethylase 5C;Inhibitor of lysine demethylase 6A;Inhibitor of lysine demethylase 6B
GSK-J4 - ≥98%, high purity , CAS No.1373423-53-0, Inhibitor of lysine demethylase 5B;Inhibitor of lysine demethylase 5C;Inhibitor of lysine demethylase 6A;Inhibitor of lysine demethylase 6B
GSK-J4 is cell permeable prodrug rapidly hydrolysed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that o
Storage Temp
Store at -20°C,Desiccated
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of lysine demethylase 5B;Inhibitor of lysine demethylase 5C;Inhibitor of lysine demethylase 6A;Inhibitor of lysine demethylase 6B
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Product Application:
GSK-J4 has been used to study the effect of KDM2B (Jumonji (JmjC) domain histone 3 lysine 36 (H3K36) di-demethylase) inhibition on the survival and DNA repair potential of glioblastoma cells. It has also been used in sulforhodamine B (SRB) cell growth assay and cell viability assay.
1.Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H et al.. (2012) A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.. Nature, 488 (7411):(404-8). [PMID:22842901][10.1021/op500134e]
2.Heinemann B, Nielsen JM, Hudlebusch HR, Lees MJ, Larsen DV, Boesen T, Labelle M, Gerlach LO, Birk P, Helin K. (2014) Inhibition of demethylases by GSK-J1/J4.. Nature, 514 (7520):(E1-2). [PMID:25279926][10.1021/op500134e]
3.Cribbs A, Hookway ES, Wells G, Lindow M, Obad S, Oerum H, Prinjha RK, Athanasou N, Sowman A, Philpott M et al.. (2018) Inhibition of histone H3K27 demethylases selectively modulates inflammatory phenotypes of natural killer cells.. J Biol Chem, 293 (7):(2422-2437). [PMID:29301935][10.1021/op500134e]
4.Gao Y et al.. (2022) H3K27 tri-demethylase JMJD3 inhibits macrophage apoptosis by promoting ADORA2A in lipopolysaccharide-induced acute lung injury.. Cell Death Discov, 8 (475). [PMID:36456564]
5.Yamada T et al.. (2019) Histone H3K27 Demethylase Negatively Controls the Memory Formation of Antigen-Stimulated CD8+ T Cells.. J Immunol, 202 (4):(1088-1098). [PMID:30626691]
6.Watarai H et al.. (2016) Impact of H3K27 Demethylase Inhibitor GSKJ4 on NSCLC Cells Alone and in Combination with Metformin.. Anticancer Res, 36 (11):(6083-6092). [PMID:27793936]
7.Sun J et al.. (2021) microRNA-27b shuttled by mesenchymal stem cell-derived exosomes prevents sepsis by targeting JMJD3 and downregulating NF-?B signaling pathway.. Stem Cell Res Ther, 12 (14). [PMID:33413595]
8.Zhang YX et al.. (2018) The histone demethylase KDM6B in the medial prefrontal cortex epigenetically regulates cocaine reward memory.. Neuropharmacology, 141 (113-125). [PMID:30165076]
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