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Submit ReviewESI 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.
分子量 | 392.28 |
公式 | C18H17N5O.2HCl |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 39.23 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: ESI 1, ESI 1 supplier, , Tocris Bioscience
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