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ESI 1

Catalog #: 8811 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
8811/10
8811/50

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ESI 1 | Class I Histone Deacetylases Inhibitors
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Description: Selective HDAC3 inhibitor; also myelination inducer

Chemical Name: N-(2-Aminophenyl)-5-[(phenylmethyl)amino]-2-pyrazinecarboxamide dihydrochloride

Purity: ≥98%

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Biological Activity

ESI 1 (epigenetic silencing inhibitor 1; also called PT3) is an HDAC3 inhibitor (IC50 = 250 nM). ESI 1 exhibits high selectivity for HDAC3 over HDAC1, HDAC6, and HDAC8. Also, ESI 1 promotes remyelination in demyelinated animal models and enables de novo myelinogenesis on regenerated CNS axons. In vivo, ESI 1 enhances long-term memory in mouse model of novel object recognition. ESI 1 triggers nuclear condensate formation of lipid-metabolic regulators SREBP1/2, concentrating transcriptional co-activators to drive lipid/cholesterol biosynthesis. ESI 1 is orally bioavailable and blood-brain-barrier penetrant.

Technical Data

M.Wt:
392.28
Formula:
C18H17N5O.2HCl
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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