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PS 1145 dihydrochloride is a selective IκB kinase (IKK) inhibitor (IC50 = 100 nM). Has no effect on PKA, PKC and CKII activity. Inhibits IκB-α phosphorylation and NFκB activation in HeLa cells. Inhibits NFκB-mediated proinflammatory gene expression in human airway epithelial cells. Enhances TNF-α-induced apoptosis in a multiple myeloma cell line. Attenuates LPS-induced TNF-α production in vivo. Orally active.
分子量 | 395.67 |
公式 | C17H11ClN4O.2HCl |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1049743-58-9 |
PubChem ID | 16219884 |
InChI Key | QTDCBADLGJZBHP-UHFFFAOYSA-N |
Smiles | ClC1=CC(NC(C4=CC=CN=C4)=O)=C(NC3=C2C=CN=C3)C2=C1.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.
参考文献是支持产品生物活性的出版物。
Castro et al (2003) Novel IKK inhibitors: beta-carbolines. Bioorg.Med.Chem.Lett. 13 2419 PMID: 12824047
Newton et al (2007) Repression of inflammatory gene expression in human pulmonary epithelial cells by small-molecule IkappaB kinase inhibitors. J.Pharmacol.Exp.Ther. 321 734 PMID: 17322026
Hideshima et al (2002) NF-kappa B as a therapeutic target in multiple myeloma. J.Biol.Chem. 277 16639 PMID: 11872748
关键词: PS 1145 dihydrochloride, PS 1145 dihydrochloride supplier, PS1145, dihydrochloride, selective, IKK, IκB, kinase, IkappaB, IKB, inhibitors, inhibits, cytokines, signaling, NFκB, NFKappaB, NFKB, TNF-alpha, TNF-a, TNF-α, orally, active, IkB, Kinase, NF-kB/IkB, 4569, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PS 1145 dihydrochloride 的部分引用包括:
Gari et al (2016) Loss of the oncogenic phosphatase PRL-3 promotes a TNF-R1 feedback loop that mediates triple-negative breast cancer growth. Oncogenesis 5 e255 PMID: 27526109
Anastasia et al (2021) The cell polarity kinase Par1b/MARK2 activation selects specific NF-kB transcripts via phosphorylation of core mediator Med17/TRAP80. Mol Biol Cell 32 690-702 PMID: 33596087
Savas et al (2022) NF-κB memory coordinates transcriptional responses to dynamic inflammatory stimuli. Cell Rep 40 111159 PMID: 35977475
L Gail et al (2022) Induction of IDO1 and Kynurenine by Serine Proteases Subtilisin, Prostate Specific Antigen, CD26 and HtrA: A New Form of Immunosuppression? Front Immunol 13 832989 PMID: 35371018
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