A pyridine regio-isomer of the JMJD3 inhibitor GSK-J4; cell-permeable and hydrolyzed to a free base

GSK-J5 (hydrochloride) – 50 mg

Brand:
Cayman
CAS:
1797983-32-4
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 (Item No. 12073) is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 (Item No. 12054), an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.{21388} However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.{21388}  

 

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SKU: 12074 - 50 mg Category:

Description

A pyridine regio-isomer of the JMJD3 inhibitor GSK-J4; cell-permeable and hydrolyzed to a free base, which is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal negative control molecule

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

Synonyms: 

Molecular weight: 454

CAS: 1797983-32-4

Purity: ≥95%

Formulation: A crystalline solid

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

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