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Cucurbitacin I

Cucurbitacin I
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Purity:98.2%
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Cucurbitacin I

Catalog No. TQ0196Cas No. 2222-07-3
Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
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Pack SizePriceAvailabilityQuantity
1 mg$77In Stock
5 mg$179In Stock
10 mg$239In Stock
25 mg$395In Stock
50 mg$588In Stock
1 mL x 10 mM (in DMSO)$198In Stock
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Product Introduction

Bioactivity
Description
Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity.
In vitro
The anticancer activity of Cucurbitacin I is accomplished by downregulating p-STAT3 and MMP-9 expression [1]. Incubation of the Seax cell line with the Jak/Stat3 inhibitor Cucurbitacin I result in a time- and concentration-dependent decrease of P-Stat3 and Stat3. Incubation of freshly isolated Sz cells with 30 μM Cucurbitacin I for 6 hours induces apoptosis in the large majority (73-91%) of tumor cells [2]. PE-induced cell enlargement and upregulation of ANF and β-MHC are significantly suppressed by pretreatment of the cardiomyocytes with Cucurbitacin I. Cucurbitacin I also impaired connective tissue growth factor (CTGF) and MAPK signaling, pro-hypertrophic factors, as well as TGF-β/Smad signaling, the important contributing factors to fibrosis [3].
In vivo
The differences in tumor volume between the Cucurbitacin I and control, combination and control, and combination and Cucurbitacin I arms are significant. Furthermore, combination-treated tumors exhibit a significantly lower average tumor weight at study termination than control. Moreover, there was no effect on the body weights of mice [4].
Animal Research
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].
AliasNSC-521777, JSI-124, Elatericin B
Chemical Properties
Molecular Weight514.65
FormulaC30H42O7
Cas No.2222-07-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 95 mg/mL (184.59 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9431 mL9.7153 mL19.4307 mL97.1534 mL
5 mM0.3886 mL1.9431 mL3.8861 mL19.4307 mL
10 mM0.1943 mL0.9715 mL1.9431 mL9.7153 mL
20 mM0.0972 mL0.4858 mL0.9715 mL4.8577 mL
50 mM0.0389 mL0.1943 mL0.3886 mL1.9431 mL
100 mM0.0194 mL0.0972 mL0.1943 mL0.9715 mL

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