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Description: Selective HDAC3 inhibitor; also myelination inducer
Chemical Name: N-(2-Aminophenyl)-5-[(phenylmethyl)amino]-2-pyrazinecarboxamide dihydrochloride
Purity: ≥98% (HPLC)
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.
| 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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Product Datasheets for ESI 1
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
If you know of a relevant reference for ESI 1, please let us know.
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Keywords: ESI 1, ESI 1 supplier, ESI, 1, ESI1, PT3, PT, 3, inhibitors, inhibits, SREBP1, SREBP2, myelin, lipid, metabolism, selective, HDAC, in, vivo, orally, bioavailable, blood, brain, barrier, penetrant, BBB, Class, I, HDACs, Neuronal, Metabolism, 8811, Tocris Bioscience
Citations for ESI 1
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
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In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.