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.

• 別名: Cucurbitacin I, Cucumis sativus L., JSI-124, STAT3 Inhibitor XIV
• 実験式（ヒル表記法）: C₃₀H₄₂O₇
• CAS番号: 2222-07-3
• 分子量: 514.65
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: ethanol: 10 mg/mL; DMSO: 100 mg/mL
• 輸送温度: ambient
• 保管温度: −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
• InChI Key: NISPVUDLMHQFRQ-MKIKIEMVSA-N

詳細

詳細

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.

生物化学的／生理学的作用

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

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

法的情報

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

安全性情報

• ピクトグラム: GHS06
• シグナルワード: Danger
• 危険有害性情報: H301
• 注意書き: P264 - P270 - P301 + P310 - P405 - P501
• 危険有害性の分類: Acute Tox. 3 Oral
• 保管分類コード: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable