JTE 607 dihydrochloride

Pricing Availability   Qty
说明: Active metabolite binds CPSF3; Pro-drug
别名: TO-207
化学名: N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride
纯度: ≥98% (HPLC)
说明书
引用文献 (3)
评论
文献 (2)

生物活性 for JTE 607 dihydrochloride

JTE 607 dihydrochloride is a pro-drug that is cleaved by carboxylesterase 1 (CES1) to its active metabolite, which then binds to cleavage and polyadenylation specificity factor 3 (CPSF3; Kd = 370 nM at human CPSF3). Treatment of A-673 cells with JTE 607 results in inhibition of mRNA cleavage and accumulation of nuclear R-loops. JTE 607 induces apoptosis in leukemia cells in vitro and prolongs survival in a mouse leukemia model. JTE 607 inhibits cytokine release and inhibits production of IL-1β, IL-8, IL-6, IL-10 and TNFα (IC50 values are 5.9, 7.3, 8.8, 9.1 and 11.0 nM, respectively) from LPS-stimulated PBMCs. In a rat model of lung injury, JTE 607 reduces proinflammatory cytokine-release and attenuates lung permeability.

化合物库 for JTE 607 dihydrochloride

JTE 607 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。

技术数据 for JTE 607 dihydrochloride

分子量 597.36
公式 C25H31Cl2N3O5.2HCl
储存 Desiccate at RT
纯度 ≥98% (HPLC)
CAS Number 188791-09-5
PubChem ID 9938544
InChI Key JUJAUEQJEWIWCQ-FJSYBICCSA-N
Smiles ClC1=C(OCCN2CCN(C)CC2)C(Cl)=CC(C(N[C@@H](CC3=CC=CC=C3)C(OCC)=O)=O)=C1O.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 JTE 607 dihydrochloride

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
water 59.74 100
DMSO 59.74 100

制备储备液 for JTE 607 dihydrochloride

以下数据基于产品分子量 597.36。 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 1.67 mL 8.37 mL 16.74 mL
5 mM 0.33 mL 1.67 mL 3.35 mL
10 mM 0.17 mL 0.84 mL 1.67 mL
50 mM 0.03 mL 0.17 mL 0.33 mL

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产品说明书 for JTE 607 dihydrochloride

分析证书/产品说明书
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参考文献 for JTE 607 dihydrochloride

参考文献是支持产品生物活性的出版物。

Kakutani et al (1999) JTE-607, a novel inflammatory cytokine synthesis inhibitor without immunosuppression, protects from endotoxin shock in mice. Inflamm.Res. 48 461 PMID: 10493164

Jian (2004) JTE-607, a cytokine release blocker, attenuates acid aspiration-induced lung injury in rats. Eur.J.Pharmacol. 488 231 PMID: 15044056

Tajima et al (2010) JTE-607, a multiple cytokine production inhibitor, induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells. Cancer Sci. 101 774 PMID: 20028380

Ross et al (2020) CPSF3-dependent pre-mRNA processing as a druggable node in AML and Ewing's sarcoma. Nat.Chem.Biol. 16 50 PMID: 31819276


If you know of a relevant reference for JTE 607 dihydrochloride, please let us know.

关键词: JTE 607 dihydrochloride, JTE 607 dihydrochloride supplier, JTE607, dihydrochloride, cytokines, inhibitors, inhibits, TNFa, TNF-alpha, TNF-α, interleukins, IL-1beta, IL-1b, IL-1β, inflammation, anti-inflammatory, IL-6, IL-8, IL-10, apoptosis, CPSF3, cleavage, and, polyadenylation, specificity, factor, 3, TO-207, Cytokines, DNA,, RNA, Protein, Synthesis, 5185, Tocris Bioscience

3 篇 JTE 607 dihydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 JTE 607 dihydrochloride 的部分引用包括:

Futami et al (2020) The novel multi-cytokine inhibitor TO-207 specifically inhibits pro-inflammatory cytokine secretion in monocytes without affecting the killing ability of CAR T cells PLoS One 15 PMID: 32320454

Nidhi et al (2021) The distinct roles of calcium in rapid control of neuronal glycolysis and the tricarboxylic acid cycle. Elife 10 PMID: 33555254

Huiyun et al (2022) Targeting the mRNA endonuclease CPSF73 inhibits breast cancer cell migration, invasion, and self-renewal. iScience 25 104804 PMID: 35992060


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