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  • JK184

    • JK 184;JK-184;Hh Signaling Antagonist VII
    货号: abs814562
    CAS号: 315703-52-7
    分子式: C19H18N4OS
    分子量: 350.44
    产品说明书
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    货号-规格 货期 价格 数量
    abs814562-5mg 1-2周 ¥582.00
    - +
    abs814562-10mg 1-2周 ¥922.00
    - +
    abs814562-25mg 1-2周 ¥2199.00
    - +
    abs814562-50mg 1-2周 ¥3638.00
    - +
    大包装询价
    产品描述
    描述

    JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    形态
    Solid
    基本信息
    别名
    JK 184;JK-184;Hh Signaling Antagonist VII
    外观
    off-white to light brown powder
    密度
    ~1.3 g/cm3 (Predicted)
    折射率
    n20D 1.68 (Predicted)
    IC50
    enzymatic activity of Adh7: IC50 = 210 nM; Hg-Ag-induced Gli-transcription activity : IC50 = 30 nM; sonic hedgehog induced Gli transcription: IC50 = 30 nM
    可溶性/溶解性
    DMSO : ≥ 50 mg/mL (142.68 mM)
    PubChem CID
    1069686
    生物活性
    靶点
    Hedgehog
    In vitro(体外研究)
    JK184 is designed to antagonize Hh signaling by inhibiting glioma (Gli)-dependent transcriptional activity in a dose dependent manner. JK184 significantly inhibitts proliferation of HUVECs with IC50 of 6.3 μg/mL after three days incubation. To evaluate anti-tumor effect of JK184, MTT assay is conducted in Panc-1 and BxPC-3 cells after administration with indicated concentrations of compounds, half maximal inhibitory concentration (IC50) of JK184 (23.7 ng/mL in anc-1 and 34.3 ng/mL in BxPC-3). Claudin-low cell lines are more sensitive to JK184 treatment than are MCF10a, MTSV1-7, or HMLE-shGFP and HMLE-pBP cells, and JK184 induced a dose-dependent decrease in glioma-associated oncogene homolog 1 (GLI1) transcript and protein levels in these cells. Treatment with the IC50 dose of JK184 enhances the proportion of HMLE-shEcad cells that stained with Annexin-V, but are negative for propidium iodide (PI) (P<0.0001, t test).
    In vivo(体内研究)
    JK184 (5 mg/kg, injected intravenously) exhibits good anti-proliferative activity in subcutaneous Panc-1 and BxPC-3 tumor models, and is a good candidate as antitumor drug targeted Hh signaling. However, JK184 has a poor pharmacokinetic profile and bioavailability.
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    • 实验方法 实验条件
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