Cucurbitacin I
Chemical Name: (9β,10α,16α,23E)-2,16,20,25-Tetrahydroxy-9-methyl-19-norlanosta-1,5,23-triene-3,11,22-trione
Purity: ≥95%
Biological Activity
Cucurbitacin 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Direct regulation of the proglucagon gene by insulin, leptin, and cAMP in embryonic versus adult hypothalamic neurons.
Mol. Endocrinol., 2102;26(8):1339-55. -
Adenosine augments IL-10-induced STAT3 signaling in M2c macrophages.
Koscso B, Csoka B, Kokai E, Nemeth Z, Pacher P, Virag L, Leibovich S, Hasko G
J Leukoc Biol, 2013;94(6):1309-15. -
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.
Nefedova et al.
Cancer Res., 2005;65:9525 -
Role of signal transducer and activator of transcription-3 in OE-mediated neuroprotection.
Dziennis et al.
J.Neurosci., 2007;27:7268 -
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.
Blaskovich et al.
Cancer Res., 2003;63:1270
Product Datasheets
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Citations for Cucurbitacin I
The citations listed below are publications that use Tocris products. Selected citations for Cucurbitacin I include:
8 Citations: Showing 1 - 8
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Butyrate Produced by Commensal Bacteria Down-Regulates Indolamine 2,3-Dioxygenase 1 (IDO-1) Expression via a Dual Mechanism in Human Intestinal Epithelial Cells.
Authors: Martin-Gallausiaux Et al.
Front Immunol 2019;9:2838
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Crosstalk between bone marrow-derived myofibroblasts and gastric cancer cells regulates cancer stemness and promotes tumorigenesis.
Authors: Zhu Et al.
Oncogene 2016;35:5388
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Upregulation of Nicotinic Acetylcholine Receptor α4+β2 through a Ligand-Independent PI3Kβ Mechanism That Is Enhanced by TNFα and the Jak2/p38Mapk Pathways.
Authors: Rogers and Gahring
Cell Rep 2015;10:e0143319
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Retinal injury, growth factors, and cytokines converge on β-catenin and pStat3 signaling to stimulate retina regeneration.
Authors: Wan Et al.
J Neurosci 2014;9:285
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On-target JAK2/STAT3 inhibition slows disease progression in orthotopic xenografts of human glioblastoma brain tumor stem cells.
Authors: Stechishin Et al.
Neuro Oncol 2013;15:198
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Cytokine induction of tumor necrosis factor receptor 2 is mediated by STAT3 in colon cancer cells.
Authors: Hamilton Et al.
Mol Cancer Res 2011;9:1718
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The histone deacetylase inhibitors vorin. and romid. downmodulate IL-10 expression in cutaneous T-cell lymphoma cells.
Authors: Tiffon Et al.
Br J Pharmacol 2011;162:1590
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Balancing inflammation and tolerance in vivo through dendritic cells by the commensal Candida albicans.
Authors: Bonifazi Et al.
Mucosal Immunol 2009;2:362
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