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Submit ReviewJTE 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.
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。
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 59.74 | 100 | |
DMSO | 59.74 | 100 |
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.
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 |
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
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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