HDAC1/MAO-B-IN-1

Names

[ CAS No. ]:
2759855-37-1

[ Name ]:
HDAC1/MAO-B-IN-1

Biological Activity

[Description]:

HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease[1].

[Related Catalog]:

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

[Target]

HDAC1:21.4 nM (IC50)

MAO-B:99.0 nM (IC50)


[In Vitro]

HDAC1/MAO-B-IN-1 (compound 1f) shows inhibitory activities with IC50s of 99.0 nM, 9923.0 nM, 21.4 nM for hMAO-B, hMAO-A, hHDAC1, respectively[1]. HDAC1/MAO-B-IN-1 (50 µM; 24 h) displays neuroprotective and inhibitory activity on ROS production in PC12 cells[1]. Cell Viability Assay[1] Cell Line: PC12 cells Concentration: 50 µM Incubation Time: 24 h Result: Displayed neuroprotective and inhibitory activity on ROS production.

[In Vivo]

HDAC1/MAO-B-IN-1 (20 mg/kg; i.g.) exhibits favorable BBB (blood–brain barrier) permeability[1]. HDAC1/MAO-B-IN-1 (15 mg/kg; i.p.) improves the learning and memory abilities of the ICR mice[1]. Animal Model: 6-8 weeks, ICR male mice[1] Dosage: 20 mg/kg Administration: I.g. Result: Exhibited favorable BBB (blood–brain barrier) permeability. Animal Model: 20-25 g, ICR female mice[1] Dosage: 15 mg/kg Administration: I.p.; 15 consecutive days Result: Improved the learning and memory abilities of the ICR mice.

[References]

[1]. Yao C, et al. HDAC1/MAO-B dual inhibitors against Alzheimer's disease: Design, synthesis and biological evaluation of N-propargylamine-hydroxamic acid/o-aminobenzamide hybrids. Bioorg Chem. 2022; 122:105724.

Chemical & Physical Properties

[ Molecular Formula ]:
C18H17ClN2O2

[ Molecular Weight ]:
328.79


Related Compounds