An ethyl ester prodrug of the JMJD3 selective histone demethylase inhibitor GSK-J1; reduces LPS-induced proinflammatory cytokine production

GSK-J4 (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
1797983-09-5
Storage:
-20
UN-No:
Non-Hazardous - /

The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).{21388}  

 

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SKU: 12073 - 10 mg Category:

Description

An ethyl ester prodrug of the JMJD3 selective histone demethylase inhibitor GSK-J1; reduces LPS-induced proinflammatory cytokine production, including that of TNFα (IC50 = 9 µM) in human primary macrophages

Formal name: N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine, ethyl ester, monohydrochloride

Synonyms: 

Molecular weight: 454

CAS: 1797983-09-5

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Demethylation||Research Area|Immunology & Inflammation|Innate Immunity

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