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Rodin-A

Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC) -co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease[1].

Product Specifications

CAS Number

[2222756-46-7]

UNSPSC

12352005

Target

HDAC

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Smiles

O=C(N1CC2=NC(C)=NC=C2C1)NC3=NC(C4=CC=CS4)=CC=C3N

Molecular Formula

C17H16N6OS

Molecular Weight

352.41

References & Citations

[1]Fuller NO, et al. CoREST Complex-Selective Histone Deacetylase Inhibitors Show Prosynaptic Effects and an Improved Safety Profile To Enable Treatment of Synaptopathies. ACS Chem Neurosci. 2019 Mar 20;10 (3) :1729-1743.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Curated Selection

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