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Submit ReviewCucurbitacin I is a selective inhibitor of STAT3/JAK2 signaling. Inhibits the activation of STAT3 and JAK2 and displays no activity on Src, Akt, ERK and JNK. Suppresses phosphotyrosine levels of STAT3, inhibits STAT3 DNA binding and STAT3-mediated gene expression. Induces apoptosis in cell lines expressing constitutively active tyrosine-phosphorylated STAT3.
分子量 | 514.65 |
公式 | C30H42O7 |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 2222-07-3 |
PubChem ID | 5281321 |
InChI Key | NISPVUDLMHQFRQ-MKIKIEMVSA-N |
Smiles | OC(C)(C)/C=C/C([C@@](O)(C)[C@@]3([H])[C@H](O)C[C@@]([C@@](C)3C4)(C)[C@]2([H])CC=C1C(C)(C)C(C(O)=C[C@]([H])1[C@@](C)2C4=O)=O)=O |
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 | 5.15 | 10 |
以下数据基于产品分子量 514.65。 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 |
---|---|---|---|
0.1 mM | 19.43 mL | 97.15 mL | 194.31 mL |
0.5 mM | 3.89 mL | 19.43 mL | 38.86 mL |
1 mM | 1.94 mL | 9.72 mL | 19.43 mL |
5 mM | 0.39 mL | 1.94 mL | 3.89 mL |
参考文献是支持产品生物活性的出版物。
Blaskovich et al (2003) Discovery of JSI-124 (cucurbitacin I), a selective janus kinase/signal transducer and activator of transcription 3 signaling pathway inhibitor with potent antitumor activity against human and murine cancer cells in mice. Cancer Res. 63 1270 PMID: 12649187
Nefedova et al (2005) Regulation of dendritic cell differentiation and antitumor immune response in cancer by pharmacologic-selective inhibition of the janus-activated kinase 2/signal transducers and activators of transcription 3 pathway. Cancer Res. 65 9525 PMID: 16230418
Dziennis et al (2007) Role of signal transducer and activator of transcription-3 in OE-mediated neuroprotection. J.Neurosci. 27 7268 PMID: 17611279
If you know of a relevant reference for Cucurbitacin I, please let us know.
关键词: Cucurbitacin I, Cucurbitacin I supplier, Selective, inhibitors, inhibits, STAT3/JAK2, signaling, signalling, Janus, Activated, Kinase, JAK, Kinases, Signal, Transducers, activators, Transcription, STAT, CucurbitacinI, ElatericinB, JSI124, Elatericin, B, JSI, 124, 1571, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Cucurbitacin I 的部分引用包括:
Martin-Gallausiaux et al (2019) Butyrate Produced by Commensal Bacteria Down-Regulates Indolamine 2,3-Dioxygenase 1 (IDO-1) Expression via a Dual Mechanism in Human Intestinal Epithelial Cells. Front Immunol 9 2838 PMID: 30619249
Hamilton et al (2011) Cytokine induction of tumor necrosis factor receptor 2 is mediated by STAT3 in colon cancer cells. Mol Cancer Res 9 1718 PMID: 21994466
Rogers and Gahring (2015) Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways. Cell Rep 10 e0143319 PMID: 26619345
Wan et al (2014) Retinal injury, growth factors, and cytokines converge on β-catenin and pStat3 signaling to stimulate retina regeneration. J Neurosci 9 285 PMID: 25263555
Stechishin et al (2013) On-target JAK2/STAT3 inhibition slows disease progression in orthotopic xenografts of human glioblastoma brain tumor stem cells. Neuro Oncol 15 198 PMID: 23262510
Tiffon et al (2011) The histone deacetylase inhibitors vorin. and romid. downmodulate IL-10 expression in cutaneous T-cell lymphoma cells. Br J Pharmacol 162 1590 PMID: 21198545
Bonifazi et al (2009) Balancing inflammation and tolerance in vivo through dendritic cells by the commensal Candida albicans. Mucosal Immunol 2 362 PMID: 19421183
Zhu et al (2016) Crosstalk between bone marrow-derived myofibroblasts and gastric cancer cells regulates cancer stemness and promotes tumorigenesis. Oncogene 35 5388 PMID: 27109105
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