ESI 1
Tocris Bioscience, part of Bio-Techne | Catalog # 8811
Selective HDAC3 inhibitor; also myelination inducer
Key Product Details
Description
Selective HDAC3 inhibitor; also myelination inducer
Product Description
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.Product Specifications
Molecular Weight
392.28
Formula
C18H17N5O.2HCl
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
N-(2-Aminophenyl)-5-[(phenylmethyl)amino]-2-pyrazinecarboxamide dihydrochloride
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.
Solubility
| 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 all 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 | 5.10 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.55 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Pulya PT3: A novel benzamide class histone deacetylase 3 inhibitor improves learning and memory in novel object recognition mouse model. ACS Chem.Neurosci. 2021 PMID: 33577290
- Liu Small-molecule-induced epigenetic rejuvenation promotes SREBP condensation and overcomes barriers to CNS myelin regeneration. Cell 2024 PMID: 38701782
Product Specific Notices for ESI 1
For research use only
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