PDE5/HDAC-IN-1

Names

[ CAS No. ]:
2414921-48-3

[ Name ]:
PDE5/HDAC-IN-1

Biological Activity

[Description]:

PDE5/HDAC-IN-1 (Compound 26) is a potent phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50 values of 46.3 nM and 14.5 nM, respectively. PDE5/HDAC-IN-1 induces cell apoptosis and shows anticancer activities[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC
Signaling Pathways >> Epigenetics >> HDAC

[Target]

PDE5:46.3 nM (IC50)

HDAC1:2.45 μM (IC50)

HDAC6:0.11 μM (IC50)

HDAC8:0.12 μM (IC50)


[In Vitro]

PDE5/HDAC-IN-1 (Compound 26) shows growth inhibition with IC50 values of 12.35, 7.19 and 11.79 µM against HT-29, HCT-116 and SW-620 cells, respectively[1]. PDE5/HDAC-IN-1 shows cytotoxic activity with IC50 values of 1.9, 1.5, 2.5, 5.5, 9.8, 18.6, 2 and 28.2 μM against Molt 4, Sup-T1, K562, AGS, PC-3, LNCaP, T47D and CCD966SK, respectively[1].

[References]

[1]. ElHady AK, et al. Extending the use of tadalafil scaffold: Development of novel selective phosphodiesterase 5 inhibitors and histone deacetylase inhibitors. Bioorg Chem. 2020 May;98:103742.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H29BrN4O4

[ Molecular Weight ]:
553.45

Related Compounds