Cucurbitacin IA Stat3 and JAK2 inhibitor and antiproliferative agent

Cucurbitacin I (CAS 2222-07-3)

Cucurbitacin I | CAS 2222-07-3 is rated 5.0 out of 5 by 1.
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Synonym: Elatericin B
Application: A Stat3 and JAK2 inhibitor and antiproliferative agent
CAS Number: 2222-07-3
Purity: ≥95%
Molecular Weight: 514.65
Molecular Formula: C30H42O7
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Cucurbitacin I, Cucumis sativus L. has been found to suppress levels of phosphotyrosine Stat3 (signal transducer and activator of transcription 3) in v-Src-transformed NIH 3T3 cells. These transcription factors have been known to mediate a wide variety of biological functions in the peripheral and central nervous systems. Their inhibition can result in the suppression of Stat3 DNA binding and Stat3-mediated gene transcription. Additionally this compound has been found to reduce in vitro clonogenicity of certain cancer cells. The anti-proliferation activity of this compound is also related to its downregulating activity against Stat3 target gene expression. Hyperactivation of the JAK2 (Janus-activated kinase 2) has been reported to be responsible for abnormal dendritic cell differentiation. The blocking of this kinase by Curcurbitacin I could potentially stop abnormal dendrite cell differentiation and promote differentiation of mature macrophages and dendritic cells. Cucurbitacin I, Cucumis sativus L. is an inhibitor of JAK2.


References

1. Blaskovich, M.A., et al. 2003. Cancer Res. 63: 1270-1279. PMID: 12649187
2. Nefedova, Y., et al. 2005. Cancer Res. 65: 9525-9535. PMID: 16230418
3. Dziennis, S. and Alkayed, N.J. 2008. Rev Neurosci. 19: 341-361. PMID: 19145989
4. Lui, V.W., et al. 2009. Carcinogenesis. 30: 2085-2094. PMID: 19843642

Physical State :
Solid
Derived From :
Cucumis sativus L.
Solubility :
Soluble in DMSO (10 mM), and ethanol (20 mM).
Storage :
Desiccate at -20° C
Boiling Point :
698.32° C at 760 mmHg (Predicted)
Density :
1.26 g/cm3 (Predicted)
Refractive Index :
n20D 1.59 (Predicted)
IC50 :
HL-60: IC50 = 0.1 nM (human); U-937: IC50 = 0.3 nM (human); HT-1080: IC50 = 0.47 nM (human); HT-29: IC50 = 190 nM (human); Integrin αL: IC50 = 950 nM (human)
pK Values :
pKa: 8.51 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
RC6200000
PubChem CID :
5281321
MDL Number :
MFCD09971044
EC Number :
218-736-8
SMILES :
C[C@@]12C[C@H]([C@@H]([C@]1(CC(=O)[C@@]3([C@H]2CC=C4[C@H]3C=C(C(=O)C4(C)C)O)C)C)[C@](C)(C(=O)/C=C/C(C)(C)O)O)O

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Cucurbitacin I  Product Citations

See how others have used Cucurbitacin I. Click on the entry to view the PubMed entry .

Citations 1 to 6 of 6 total

PMID: # 30776726  Panek, CA.|Bruballa, AC.|Pineda, GE.|De Brasi, C.|Fernández-Brando, RJ.|Mejías, MP.|Ramos, MV.|Palermo, MS.| et al. 2019. Mol. Immunol. 108: 23-33.

PMID: # 24733676  Kim, HJ. et al. 2015. Archives of pharmacal research. 38: 290-8.

PMID: # 25571964  Zhang, N. et al. 2015. Oncology reports. 33: 1493-8.

PMID: # 25047252  Wu, T. et al. 2014. 66: 3129-39.

PMID: # 24858077  Kim, HJ. et al. 2014. Chemico-biological interactions. 219: 1-8.

PMID: # 22450744  Ozenne, P. et al. 2013. Oncogene. 32: 1050-8.

Citations 1 to 6 of 6 total
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Rated 5 out of 5 by from Jeong Jeong, MH. et al. (PubMed 26296085) evaluated the functional role of Cucurbitacin I, a Stat3 and JAK2 inhibitor, in an in vitro model of cardiac hypertrophy. Found cardioprotective effects via inhibition of CTGF/MAPK, and TGF- /Smad-facilitated events. -SCBT Publication Review
Date published: 2015-07-06
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