1. Immunology/Inflammation Apoptosis
  2. Interleukin Related Apoptosis
  3. SC144

SC144 是首创的口服活性 gp130 (IL6-beta) 抑制剂。SC144 结合 gp130,诱导 gp130 磷酸化(S782) 和去糖基化,消除 Stat3 磷酸化和核易位,进一步抑制下游靶基因的表达。SC144 对 gp130 配体触发的信号转导有明显的抑制作用。SC144 诱导人卵巢癌细胞凋亡。

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SC144 Chemical Structure

SC144 Chemical Structure

CAS No. : 895158-95-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥605
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1 mg ¥250
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5 mg ¥550
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10 mg ¥935
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25 mg ¥1825
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50 mg ¥3063
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100 mg ¥4900
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500 mg   询价  

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Top Publications Citing Use of Products

    SC144 purchased from MCE. Usage Cited in: Inflamm Res. 2023 Jan 8.  [Abstract]

    SC144 (20 mg/kg; dissolved in DMSO; i.p.; single) significantly inhibits the expression of gp130 in mouse lung tissue.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells[1].

    IC50 & Target[1]

    IL6-beta

     

    体外研究
    (In Vitro)

    SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC50s in a submicromolar range (IC50=OVCAR-8, OVCAR-5, OVCAR-3= 0.72, 0.49, 0.95 μM)[1].
    ? The potency of SC144 toward NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC50=0.43 μM) and HEY (Cisplatin-resistant, IC50=0.88 μM) suggests an ability to overcome drug resistance in ovarian cancer[1].
    ? SC144 (2 μM; 24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells[1].
    ? SC144 (0.5-2 μM; 0-6 hours) substantially increases the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time- and dose-dependent manner[1].
    ? SC144 is cytotoxic to ovarian cancer cells via a mechanism involving the inhibition of gp130 activity, leading to the inactivation of Akt and Stat3 as well as the suppression of Stat3-regulated gene expression. As are result, SC144 treatment eventually causes cell-cycle arrest, anti-angiogenesis, and apoptosis[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Apoptosis Analysis[1]

    Cell Line: OVCAR-8 and Caov-3 cells
    Concentration: 2 μM
    Incubation Time: 24 hours
    Result: Significantly caused cell death in OVCAR-8 and Caov-3 cells.

    Western Blot Analysis[1]

    Cell Line: OVCAR-8, Caov-3 cells
    Concentration: 0.5-2 μM
    Incubation Time: 0-6 hours
    Result: Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner.
    体内研究
    (In Vivo)

    SC144 (10 mg/kg; i.p.; daily for 58 days) suppresses tumor growth in human ovariancancer xenografts[1].
    ? SC144 (100 mg/kg;p.o.; daily for 35 days) treatment shows the average tumor volume in mice 82% smaller than that in the control group[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Athymic mice (human ovarian cancer xenograft)[1]
    Dosage: 10 mg/kg
    Administration: I.p; daily for 58 days
    Result: Significantly inhibited tumor growth by about 73%.
    分子量

    322.30

    Formula

    C16H11FN6O

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 16.67 mg/mL (51.72 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.1027 mL 15.5135 mL 31.0270 mL
    5 mM 0.6205 mL 3.1027 mL 6.2054 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料
    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.1027 mL 15.5135 mL 31.0270 mL 77.5675 mL
    5 mM 0.6205 mL 3.1027 mL 6.2054 mL 15.5135 mL
    10 mM 0.3103 mL 1.5513 mL 3.1027 mL 7.7567 mL
    15 mM 0.2068 mL 1.0342 mL 2.0685 mL 5.1712 mL
    20 mM 0.1551 mL 0.7757 mL 1.5513 mL 3.8784 mL
    25 mM 0.1241 mL 0.6205 mL 1.2411 mL 3.1027 mL
    30 mM 0.1034 mL 0.5171 mL 1.0342 mL 2.5856 mL
    40 mM 0.0776 mL 0.3878 mL 0.7757 mL 1.9392 mL
    50 mM 0.0621 mL 0.3103 mL 0.6205 mL 1.5513 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    SC144
    目录号:
    HY-15614
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