CUCURBITACIN I
Synonym(s):2,16α,20,25-Tetrahydroxy-9-methyl-19-Nor-9β,10α-lanosta-1,5,23-triene-3,11,22-trione;Elatericin B;JSI-124;NSC 521777
- CAS NO.:2222-07-3
- Empirical Formula: C30H42O7
- Molecular Weight: 514.65
- MDL number: MFCD09971044
- EINECS: 218-736-8
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-04 20:04:50
What is CUCURBITACIN I?
The Uses of CUCURBITACIN I
Cucurbitacin I can be useful in the study of edible vitalmelon fruit extract and adipogenesis.
What are the applications of Application
Cucurbitacin I is a Stat3 and JAK2 inhibitor and antiproliferative agent
Definition
ChEBI: A cucurbitacin that is 9,10,14-trimethyl-4,9-cyclo-9,10-secocholesta-2,5,23-triene substituted by hydroxy groups at positions 2, 16, 20 and 25 and oxo groups at positions 1, 11 and 22.
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.
Biochem/physiol Actions
Cucurbitacin I (JSI-124) is a novel selective inhibitor of the janus kinase 2/signal transducer and activator of transcription 3 (JAK2/STAT3) signaling pathway with anti-proliferative and anti-tumor properties.
storage
Store at -20°C
References
blaskovich ma, sun j, cantor a et al. 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. 2003 mar 15;63(6):1270-9.yu h, lee h, herrmann a et al. revisiting stat3 signalling in cancer: new and unexpected biological functions.nat rev cancer. 2014 nov;14(11):736-46. doi: 10.1038/nrc3818.song j, liu h, li z et al. cucurbitacin i inhibits cell migration and invasion and enhances chemosensitivity in colon cancer. oncol rep. 2015 apr;33(4):1867-71. qi j, xia g, huang cr et al. jsi-124 (cucurbitacin i) inhibits tumor angiogenesis of human breast cancer through reduction of stat3 phosphorylation. am j chin med. 2015;43(2):337-47.kim hj, kim jk et al. antiangiogenic effects of cucurbitacin-i. arch pharm res. 2015 feb;38(2):290-8. yuan g, yan sf, xue h et al. cucurbitacin i induces protective autophagy in glioblastoma in vitro and in vivo. j biol chem. 2014 apr 11;289(15):10607-19.
Properties of CUCURBITACIN I
Melting point: | 148-150°C |
Boiling point: | 698.3±55.0 °C(Predicted) |
Density | 1.26±0.1 g/cm3(Predicted) |
storage temp. | -20°C |
solubility | ≥22.45 mg/mL in DMSO; insoluble in EtOH; ≥51.2 mg/mL in H2O with ultrasonic |
pka | 8.51±0.70(Predicted) |
form | solid |
color | white to off-white |
Safety information for CUCURBITACIN I
Signal word | Danger |
Pictogram(s) |
Skull and Crossbones Acute Toxicity GHS06 |
GHS Hazard Statements |
H301:Acute toxicity,oral |
Computed Descriptors for CUCURBITACIN I
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