HDAC6-IN-5

Names

[ CAS No. ]:
2413603-15-1

[ Name ]:
HDAC6-IN-5

Biological Activity

[Description]:

HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity[1].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC
Research Areas >> Neurological Disease
Signaling Pathways >> Epigenetics >> HDAC
Signaling Pathways >> Neuronal Signaling >> AChE

[Target]

HDAC6:0.026 ± 0. μM (IC50)

HDAC1:0.09 ± 0.0 μM (IC50)

HDAC:0.16 ± 0.0 μM (IC50)

HDAC3:0.33 ± 0. μM (IC50)

HDAC2:0.48 ± 0.0 μM (IC50)

HDAC9:5.51 ± 0.0 μM (IC50)

HDAC5:7.19 ± 0.4 μM (IC50)

HDAC4:7.85 ± 0.6 μM (IC50)

HDAC7:9.13 ± 0.3 μM (IC50)


[In Vitro]

HDAC6-IN-5 (compound 11b) induces histone H3 and α-tubulin acetylation in a dose-dependent manner, with EC50 values of 0.58 and 8 μM, respectively[1]

[References]

[1]. Tseng HJ, et al. Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease. Eur J Med Chem. 2020 Apr 15;192:112193.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H14BrN3O2

[ Molecular Weight ]:
408.25

Related Compounds