product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
4594/10
catalog :
4594/10
quantity :
10 mg (also 50 mg)
price :
254 USD
more info or order :
citations: 23
Reference
Hung P, Hsu Y, Chen T, Ho C, Lin C. The Histone Demethylase Inhibitor GSK-J4 Is a Therapeutic Target for the Kidney Fibrosis of Diabetic Kidney Disease via DKK1 Modulation. Int J Mol Sci. 2022;23: pubmed publisher
Song Y, Hou G, Diep J, Ooi Y, Akopyants N, Beverley S, et al. Inhibitor of growth protein 3 epigenetically silences endogenous retroviral elements and prevents innate immune activation. Nucleic Acids Res. 2021;49:12706-12715 pubmed publisher
Lunazzi G, Buxade M, Riera Borrull M, Higuera L, Bonnin S, Huerga Encabo H, et al. NFAT5 Amplifies Antipathogen Responses by Enhancing Chromatin Accessibility, H3K27 Demethylation, and Transcription Factor Recruitment. J Immunol. 2021;206:2652-2667 pubmed publisher
Davis F, Tsoi L, Melvin W, denDekker A, Wasikowski R, Joshi A, et al. Inhibition of macrophage histone demethylase JMJD3 protects against abdominal aortic aneurysms. J Exp Med. 2021;218: pubmed publisher
Riching A, Danis E, Zhao Y, Cao Y, Chi C, Bagchi R, et al. Suppression of canonical TGF-β signaling enables GATA4 to interact with H3K27me3 demethylase JMJD3 to promote cardiomyogenesis. J Mol Cell Cardiol. 2021;153:44-59 pubmed publisher
Browning L, Miller C, Kuczma M, Pietrzak M, Jing Y, Rempala G, et al. Bone Morphogenic Proteins Are Immunoregulatory Cytokines Controlling FOXP3+ Treg Cells. Cell Rep. 2020;33:108219 pubmed publisher
Davis F, denDekker A, Joshi A, Wolf S, Audu C, Melvin W, et al. Palmitate-TLR4 signaling regulates the histone demethylase, JMJD3, in macrophages and impairs diabetic wound healing. Eur J Immunol. 2020;50:1929-1940 pubmed publisher
Nikolaev A, Fiveash J, Yang E. Combined Targeting of Mutant p53 and Jumonji Family Histone Demethylase Augments Therapeutic Efficacy of Radiation in H3K27M DIPG. Int J Mol Sci. 2020;21: pubmed publisher
Backe M, Jin C, Andreone L, Sankar A, Agger K, Helin K, et al. The Lysine Demethylase KDM5B Regulates Islet Function and Glucose Homeostasis. J Diabetes Res. 2019;2019:5451038 pubmed publisher
Lin C, Hsu Y, Huang Y, Shih Y, Wang C, Chiang W, et al. A KDM6A-KLF10 reinforcing feedback mechanism aggravates diabetic podocyte dysfunction. EMBO Mol Med. 2019;11: pubmed publisher
Bayo J, Tran T, Wang L, Peña Llopis S, Das A, Martinez E. Jumonji Inhibitors Overcome Radioresistance in Cancer through Changes in H3K4 Methylation at Double-Strand Breaks. Cell Rep. 2018;25:1040-1050.e5 pubmed publisher
Das A, Arifuzzaman S, Yoon T, Kim S, Chai J, Lee Y, et al. RNA sequencing reveals resistance of TLR4 ligand-activated microglial cells to inflammation mediated by the selective jumonji H3K27 demethylase inhibitor. Sci Rep. 2017;7:6554 pubmed publisher
Petruk S, Mariani S, De Dominici M, Porazzi P, Minieri V, Cai J, et al. Structure of Nascent Chromatin Is Essential for Hematopoietic Lineage Specification. Cell Rep. 2017;19:295-306 pubmed publisher
Ma K, Hung H, Svaren J. Epigenomic Regulation of Schwann Cell Reprogramming in Peripheral Nerve Injury. J Neurosci. 2016;36:9135-47 pubmed publisher
Sciacovelli M, Gonçalves E, Johnson T, Zecchini V, da Costa A, Gaude E, et al. Fumarate is an epigenetic modifier that elicits epithelial-to-mesenchymal transition. Nature. 2016;537:544-547 pubmed publisher
Palomer E, Carretero J, Benvegnù S, Dotti C, Martin M. Neuronal activity controls Bdnf expression via Polycomb de-repression and CREB/CBP/JMJD3 activation in mature neurons. Nat Commun. 2016;7:11081 pubmed publisher
Pan D, Huang L, Zhu L, Zou T, Ou J, Zhou W, et al. Jmjd3-Mediated H3K27me3 Dynamics Orchestrate Brown Fat Development and Regulate White Fat Plasticity. Dev Cell. 2015;35:568-583 pubmed publisher
Kang S, Kim S, Chai J, Kim S, Won K, Lee Y, et al. Transcriptomic Profiling and H3K27me3 Distribution Reveal Both Demethylase-Dependent and Independent Regulation of Developmental Gene Transcription in Cell Differentiation. PLoS ONE. 2015;10:e0135276 pubmed publisher
Aspuria P, Lunt S, Väremo L, Vergnes L, Gozo M, Beach J, et al. Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism. Cancer Metab. 2014;2:21 pubmed publisher
Perrigue P, Silva M, Warden C, Feng N, Reid M, Mota D, et al. The histone demethylase jumonji coordinates cellular senescence including secretion of neural stem cell-attracting cytokines. Mol Cancer Res. 2015;13:636-50 pubmed publisher
Carey B, Finley L, Cross J, Allis C, Thompson C. Intracellular α-ketoglutarate maintains the pluripotency of embryonic stem cells. Nature. 2015;518:413-6 pubmed publisher
Gallagher K, Joshi A, Carson W, Schaller M, ALLEN R, Mukerjee S, et al. Epigenetic changes in bone marrow progenitor cells influence the inflammatory phenotype and alter wound healing in type 2 diabetes. Diabetes. 2015;64:1420-30 pubmed publisher
Petruk S, Black K, Kovermann S, Brock H, Mazo A. Stepwise histone modifications are mediated by multiple enzymes that rapidly associate with nascent DNA during replication. Nat Commun. 2013;4:2841 pubmed publisher
product information
master code :
4594
SKU :
4594/10
product name :
GSK J4
unit size :
10 mg (also 50 mg)
description :
Histone KDM inhibitor; cell permeable
target :
Histone Demethylase Inhibitors
category :
Small Molecules
purity :
99%
observed molecular weight :
417.5
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
GSK J4 is a histone lysine demethylase (KDM) inhibitor; blocks demethylation of histone H3K27. Attenuates lipopolysaccharide (LPS)-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 M for the inhibition of TNF release). Cell permeable. Ethyl ester derivative of GSK J1 . . Negative Control also available.
top caption :
Histone KDM inhibitor; cell permeable
extended description :
Histone KDM inhibitor; cell permeable
chemical name text :
N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]- -alanine ethyl ester
formula :
C24H27N5O2
formula text :
C24H27N5O2
cas num :
1373423-53-0
USD :
254 USD
product details :
Histone KDM inhibitor; cell permeable
storage :
Store at RT
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK