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Submit ReviewCucurbitacin I
Description: Selective inhibitor of STAT3/JAK2 signaling
Alternative Names: Elatericin B,JSI 124
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% (HPLC)
Biological Activity for Cucurbitacin I
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 for Cucurbitacin I
| M. Wt | 514.65 |
| Formula | C30H42O7 |
| Storage | Store at -20°C |
| Purity | ≥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 |
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.
Solubility Data for Cucurbitacin I
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 5.15 | 10 |
Preparing Stock Solutions for Cucurbitacin I
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for Cucurbitacin I
References for Cucurbitacin I
References are publications that support the biological activity of the product.
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.
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Keywords: 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
8 Citations for Cucurbitacin I
Citations are publications that use Tocris products. Selected citations for Cucurbitacin I include:
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
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
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
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
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
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
Do you know of a great paper that uses Cucurbitacin I from Tocris? Please let us know.
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Pathways for Cucurbitacin I
