238590
Cucurbitacin I, Cucumis sativus L.
A cell-permeable and irreversible bitter triterpenoid compound (NCI identifier: NSC 521777) that displays anti-proliferative and antitumor properties both in vitro and in vivo.
别名:
Cucurbitacin I, Cucumis sativus L., JSI-124, STAT3 Inhibitor XIV
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关于此项目
经验公式（希尔记法）:
C30H42O7
化学文摘社编号:
分子量:
514.65
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
InChI
1S/C30H42O7/c1-25(2,36)12-11-21(33)30(8,37)23-19(32)14-27(5)20-10-9-16-17(13-18(31)24(35)26(16,3)4)29(20,7)22(34)15-28(23,27)6/h9,11-13,17,19-20,23,31-32,36-37H,10,14-15H2,1-8H3/b12-11+/t17-,19-,20+,23+,27+,28-,29+,30+/m1/s1
InChI key
NISPVUDLMHQFRQ-MKIKIEMVSA-N
description
RTECS - RC6200000
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
ethanol: 10 mg/mL, DMSO: 100 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
General description
A cell-permeable and irreversible bitter triterpenoid compound (NCI identifier: NSC 521777) that exhibits anti-proliferative and anti-tumor properties both in vitro and in vivo. Acts as a potent and highly selective inhibitor of Janus kinase/Signal transducer and activator of transcription 3 (Jak/STAT3) signaling pathway. Reported to suppress STAT3 tyrosine phosphorylation in v-src-transformed NIH 3T3 cells and human lung adenocarcinoma A549 cells (IC50 = 500 nM), resulting in inhibition of STAT3 DNA-binding and STAT3-mediated gene transcription. Also shown to inhibit the growth of STAT3-transformed tumors in nude mice. Does not affect oncogenic pathways mediated by Ras, Akt1, ERK1/2, or JNK.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
JAK/STAT3
JAK/STAT3
Product does not compete with ATP.
Reversible: no
Target IC50: 500 nM suppressing STAT3 tyrosine phosphorylation in v-Src-transformed NIH 3T3 cells and human lung adenocarcinoma A549 cells
Packaging
Packaged under inert gas
Other Notes
Blaskovich, M.A., et al. 2003. Cancer Res.63, 1270.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Sonia Nasi et al.
Annals of the rheumatic diseases, 75(7), 1372-1379 (2015-08-09)
Basic calcium phosphate (BCP) crystal and interleukin 6 (IL-6) have been implicated in osteoarthritis (OA). We hypothesise that these two factors may be linked in a reciprocal amplification loop which leads to OA. Primary murine chondrocytes and human cartilage explants
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