Product Introduction
Bioactivity


英文名: Cucurbitacin I

描述: Cucurbitacin I (JSI-124) 是從曲蓮中提取的一種天然產(chǎn)物，是 JAK2/STAT3選擇性抑制劑，有抗腫瘤活性。

動(dòng)物實(shí)驗(yàn): BALB/c nude (nu/nu) female mice are used. U251 cells (5×10^6 cells in 50 μL of serum-free DMEM) are inoculated subcutaneously into the right flank of 5-week-old female mice after acclimatization for a week. Tumor growth is measured daily with calipers. When the tumors reach a mean volume of 90-120 mm3, animals are randomized into groups. In the first experiment, 16 mice are randomly assigned to Cucurbitacin I (1 mg/kg/day in 20% DMSO in PBS) or drug vehicle control (20% DMSO in PBS) and dosed intraperitoneally with 100 μL of vehicle or drug once daily for 18 days, whereas, in the second, 20 mice are assigned to four groups. Control animals receive 20% DMSO in PBS vehicle, whereas treated animals are injected with Cucurbitacin I (1 mg/kg/day) in 20% DMSO in PBS, CQ (25 mg/kg/day) in 20% DMSO in PBS, and Cucurbitacin I (1 mg/kg/day) plus CQ (25 mg/kg/day) in 20% DMSO in PBS and dosed intraperitoneally with 100 μL of vehicle or drug once daily for 15 days [4].

體外活性: Cucurbitacin I的抗癌活性通過(guò)降低p-STAT3和MMP-9的表達(dá)來(lái)實(shí)現(xiàn)[1]。將Seax細(xì)胞系與Jak/Stat3抑制劑Cucurbitacin I孵育，可以觀察到P-Stat3和Stat3的表達(dá)隨時(shí)間和濃度的增加而減少。用30 μM Cucurbitacin I孵育新鮮分離的Sz細(xì)胞6小時(shí)，能在大部分（73-91%）腫瘤細(xì)胞中誘導(dǎo)凋亡[2]。Cucurbitacin I預(yù)處理心肌細(xì)胞顯著抑制由PE引起的細(xì)胞增大以及ANF和β-MHC的上調(diào)。Cucurbitacin I還抑制了連接組織生長(zhǎng)因子（CTGF）和MAPK信號(hào)通路、促心肌肥大因子以及TGF-β/Smad信號(hào)通路，這些是纖維化的重要促進(jìn)因素[3]。

體內(nèi)活性: Cucurbitacin I與對(duì)照組、聯(lián)合治療與對(duì)照組以及聯(lián)合治療與Cucurbitacin I組之間的腫瘤體積差異顯著。此外，研究結(jié)束時(shí)，聯(lián)合治療的腫瘤平均重量顯著低于對(duì)照組。而且，對(duì)小鼠體重沒(méi)有影響[4]。

存儲(chǔ)條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 95 mg/mL (184.59 mM)


關(guān)鍵字: Janus kinase | JAK | Cucurbitacin I | NSC521777 | Inhibitor | JSI124 | JSI 124 | STAT | NSC 521777 | inhibit

相關(guān)產(chǎn)品: XL019 | JAK-IN-28 | SB1317 hydrochloride (1204918-72-8(free base)) | RO495 | Pyridone 6 | JAK2-IN-7 | Kurarinone | AZ-3 | Upadacitinib | JAK3-IN-6

相關(guān)庫(kù): Anti-Tumor Natural Product Library | Terpene Natural Product Library | Transcription Factor-Targeted Compound Library | Cancer Cell Differentiation Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library | Stem Cell Differentiation Compound Library | Natural Product Library

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