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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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
Keywords: 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, JAK, Kinase, STAT, JAK, Kinase, Tocris Bioscience
