JMJD3/HDAC-IN-1

Names

[ CAS No. ]:
2883046-06-6

[ Name ]:
JMJD3/HDAC-IN-1

Biological Activity

[Description]:

JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HADC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Histone Demethylase
Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC
Signaling Pathways >> Epigenetics >> HDAC

[Target]

IC50: 16 nM (HDAC1), 534 nM (HDAC6)[1]


[References]

[1]. Li A, et al. Design, synthesis and biological evaluation of pyrimidine base hydroxamic acid derivatives as dual JMJD3 and HDAC inhibitors. Bioorg Med Chem Lett. 2023 Oct 1;94:129466.. .  

Chemical & Physical Properties

[ Molecular Formula ]:
C21H30N6O2

[ Molecular Weight ]:
398.50

Related Compounds

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