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.

• Synonim(y): Cucurbitacin I, Cucumis sativus L., JSI-124, STAT3 Inhibitor XIV
• Wzór empiryczny (zapis Hilla): C₃₀H₄₂O₇
• Numer CAS: 2222-07-3
• Masa cząsteczkowa: 514.65
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: ethanol: 10 mg/mL; DMSO: 100 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: −20°C
• 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
• Klucz InChI: NISPVUDLMHQFRQ-MKIKIEMVSA-N

Opis

Opis ogólny

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. Acts as a potent and highly selective inhibitor of Janus kinase/signal transducer and activator of transcription 3 (JAK/STAT3) signaling pathway. It suppresses 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. Shown to inhibit the growth of STAT3-transformed tumors in nude mice. Does not affect oncogenic pathways mediated by Ras, Akt, Erk1/2, or JNK.

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
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

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Inne uwagi

Blaskovich, M.A., et al. 2003. Cancer Res.63, 1270.

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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Informacja o środkach bezpieczeństwa

• Piktogramy: GHS06
• Hasło ostrzegawcze: Danger
• Zwroty wskazujące rodzaj zagrożenia: H301
• Zwroty wskazujące środki ostrożności: P264 - P270 - P301 + P310 - P405 - P501
• Klasyfikacja zagrożeń: Acute Tox. 3 Oral
• Kod klasy składowania: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable