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ESI 1

Cat. No. 8811 Submit a Review Datasheet / COA / SDS
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Chemical Name: N-(2-Aminophenyl)-5-[(phenylmethyl)amino]-2-pyrazinecarboxamide dihydrochloride
Purity: ≥98% (HPLC)
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for ESI 1

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 for ESI 1

M. Wt 392.28
Formula C18H17N5O.2HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
InChI Key PHUZJTCXTQYROR-UHFFFAOYSA-N
Smiles O=C(C1=CN=C(NCC2=CC=CC=C2)C=N1)NC3=C(N)C=CC=C3.Cl.Cl

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.

Solubility Data for ESI 1

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.23 100

Preparing Stock Solutions for ESI 1

The following data is based on the product molecular weight 392.28. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.55 mL 12.75 mL 25.49 mL
5 mM 0.51 mL 2.55 mL 5.1 mL
10 mM 0.25 mL 1.27 mL 2.55 mL
50 mM 0.05 mL 0.25 mL 0.51 mL

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References for ESI 1

References are publications that support the biological activity of the product.

Liu et al (2024) Small-molecule-induced epigenetic rejuvenation promotes SREBP condensation and overcomes barriers to CNS myelin regeneration. Cell 187 2465 PMID: 38701782

Pulya et al (2021) PT3: A novel benzamide class histone deacetylase 3 inhibitor improves learning and memory in novel object recognition mouse model. ACS Chem.Neurosci. 12 883 PMID: 33577290

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Keywords: ESI 1, ESI 1 supplier, , Tocris Bioscience

Citations for ESI 1

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