ESI 1

Pricing Availability   Qty
化学名: N-(2-Aminophenyl)-5-[(phenylmethyl)amino]-2-pyrazinecarboxamide dihydrochloride
纯度: ≥98% (HPLC)
说明书
引用文献
评论

生物活性 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.

技术数据 for ESI 1

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.

溶解性数据 for ESI 1

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 39.23 100

制备储备液 for ESI 1

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.

选择批次从而根据批次分子量重新计算:
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

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参考文献 for ESI 1

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


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关键词: ESI 1, ESI 1 supplier, , Tocris Bioscience

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