Cucurbitacin I

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Cat.No. 1571 - Cucurbitacin I | C30H42O7 | CAS No. 2222-07-3
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: ≥98% (HPLC)
Datasheet
Citations (4)
Reviews
Literature
Pathways

Biological Activity

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

M. Wt 514.65
Formula C30H42O7
Storage Store at -20°C
Purity ≥98% (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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 5.15 10
ethanol 10.29 20

Preparing Stock Solutions

The following data is based on the product molecular weight 514.65. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.94 mL 9.72 mL 19.43 mL
5 mM 0.39 mL 1.94 mL 3.89 mL
10 mM 0.19 mL 0.97 mL 1.94 mL
50 mM 0.04 mL 0.19 mL 0.39 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 estradiol-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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4 Citations for Cucurbitacin I

Citations are publications that use Tocris products. Selected citations for Cucurbitacin I include:

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

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


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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
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Immunology

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A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
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  • Immune Cell Signaling
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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for Cucurbitacin I

JAK-STAT

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.