HDAC-IN-56

Names

[ CAS No. ]:
2814571-89-4

[ Name ]:
HDAC-IN-56

Biological Activity

[Description]:

HDAC-IN-56 ((S)-17b) is an orally active class I histone deacetylase (HDAC) inhibitor with IC50 values of 56.0 ± 6.0, 90.0 ± 5.9, 422.2 ± 105.1, >10000 nM for HDAC1, HDAC2, HDAC3, and HDAC4-11, respectively. HDAC-IN-56 has potent inhibitory activity while strongly increasing intracellular levels of acetylhistone H3 and P21 and effectively inducing G1 cell cycle arrest and apoptosis.HDAC-IN-56 has antitumor activity [1].

[Related Catalog]:

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

[Target]

HDAC1:56.0 nM (IC50)

HDAC2:90.0 nM (IC50)

HDAC3:422.2 nM (IC50)


[References]

[1]. Li D, et al. Discovery of (S)-N-(2-Amino-4-fluorophenyl)-4-(1-(3-(4-((dimethylamino)methyl)phenyl)-6-oxopyridazin-1(6H)-yl)ethyl) benzamide as Potent Class I Selective HDAC Inhibitor for Oral Anticancer Drug Candidate. J Med Chem. 2023 May 25;66(10):7016-7037.  

Chemical & Physical Properties

[ Molecular Formula ]:
C28H28FN5O2

[ Molecular Weight ]:
485.55


Related Compounds