1. PI3K/Akt/mTOR Stem Cell/Wnt Cell Cycle/DNA Damage Apoptosis
  2. GSK-3 CDK Apoptosis
  3. GSK 3 Inhibitor IX

GSK 3 Inhibitor IX  (Synonyms: 6-Bromoindirubin-3'-oxime; BIO; MLS 2052)

目录号: HY-10580 纯度: 99.74%
COA 产品使用指南

GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) 是一种有效的,选择性的,可逆的,ATP 竞争性的 GSK-3α/βCDK1-cyclinB 复合体抑制剂,能够抑制 (GSK-3α/β)/CDK1/CDK5 的活性,IC50 值分别为 5 nM/320 nM/83 nM。

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GSK 3 Inhibitor IX Chemical Structure

GSK 3 Inhibitor IX Chemical Structure

CAS No. : 667463-62-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥935
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1 mg ¥403
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5 mg ¥850
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10 mg ¥1200
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50 mg ¥4500
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    GSK 3 Inhibitor IX purchased from MCE. Usage Cited in: Mol Cell Endocrinol. 2016 May 15;427:33-44.  [Abstract]

    Immunohistochemistry analyses of gene expression in the in vitro cultured tilapia ovaries obtained from 20 and 180 dah XX fish. The ovaries are cultured with or without Dkk1 and Bio.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.

    IC50 & Target[1]

    GSK-3α

    5 nM (IC50)

    GSK-3β

    5 nM (IC50)

    CDK5/p35

    80 nM (IC50)

    Cdk1/cyclin B

    320 nM (IC50)

    cdk2/cyclin A

    300 nM (IC50)

    Cdk4/cyclin D1

    10 μM (IC50)

    MAPKK

    10 μM (IC50)

    protein kinase Cα

    12 μM (IC50)

    体外研究
    (In Vitro)

    GSK 3 Inhibitor IX (BIO) 是糖原合酶激酶 3 (GSK-3) 的特异性抑制剂,对 GSK-3α/β 的 IC50 为 5 nM,选择性比 CDK5 高。
    GSK 3 Inhibitor IX 在这些激酶的 ATP 结合口袋内相互作用,降低细胞模型中 GSK-3 特异性位点上的 β-连环蛋白磷酸化,与爪蟾胚胎中的 Wnt 信号非常相似[1]
    在人类和小鼠胚胎干细胞中,GSK 3 Inhibitor IX (BIO) 维持未分化表型并维持多能状态特异性转录因子 Oct-3/4、Rex-1 和 Nanog 的表达。 GSK 3 抑制剂 IX (BIO) 介导的 Wnt 激活在功能上是可逆的,因为撤除该化合物会导致人和小鼠胚胎干细胞的正常多分化程序[2]
    GSK 3 Inhibitor IX (BIO) 促进哺乳动物心肌细胞增殖[3]
    GSK 3 Inhibitor IX (BIO) 也是一种泛 JAK 抑制剂,对 TYK2、JAK1、JAK2 和 JAK3 的 IC50 值分别为 0.03、1.5、8.0、0.5 μM。 GSK 3 Inhibitor IX (BIO) 选择性抑制 STAT3 磷酸化并诱导人黑色素瘤细胞凋亡[4]

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

    体内研究
    (In Vivo)

    GSK 3 Inhibitor IX (BIO) (50 mg/kg,口服) 抑制小鼠异种移植模型中的黑色素瘤肿瘤生长[4]

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

    Clinical Trial
    分子量

    356.17

    Formula

    C16H10BrN3O2

    CAS 号
    性状

    固体

    颜色

    Pink to red

    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 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 23 mg/mL (64.58 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.8076 mL 14.0382 mL 28.0765 mL
    5 mM 0.5615 mL 2.8076 mL 5.6153 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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 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

    纯度: 99.74%

    参考文献
    Cell Assay
    [1]

    COS1, Hepa (wild-type, CEM/LM AhR deficient and ELB1 ARNT deficient), or SH-SY5Y cells are grown in 6 cm culture dishes in Dulbecco's Modified Medium (DMEM) containing 10% fetal bovine serum. For treatment, IO (5 μM), GSK 3 Inhibitor IX (BIO) (5 or 10 μM), MeBIO (5 or 50 μM), LiCl (20 or 40 mM), or mock solution (DMSO, 0.5% final concentration) is added to medium when cell density reaches appr 70% confluence. After 12 (SH-SY5Y) or 24 hours, the cells, while still in plate, are lysed with lysis buffer (1% SDS, 1 mM sodium orthovanadate, 10 mM Tris [pH 7.4]). The lysate is passed several times through a 26G needle, centrifuged at 10,000× g for 5 min, and adjusted to equal protein concentration. About 8 μg of each sample is loaded for immunoblotting. Enhanced chemiluminescence is used for detection. The following primary antibodies are used: mouse anti-β-catenin CT, mouse anti-phospho-β-catenin, mouse anti-GSK-3 β, mouse anti-GSK-3 phosphoTyr216, rabbit anti-AhR (Aryl hydrocarbon receptor), and rabbit anti-actin.

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

    Animal Administration
    [4]

    BALB/c mice (at 6-8 weeks old) and immunodeficient NOD/SCID/IL2Rgamma null (NSG) mice (female at 6-8 weeks old) are used in the assay. A2058 human melanoma cells at 5×106 cells in serum free medium are inoculated subcutaneously into the dorsal area of NSG mice to create xenograft model. When tumors become palpable, 6 GSK 3 Inhibitor IX (BIO) or vehicle control is administered via oral gavage once daily at 50 mg/kg body weight. Tumor growth is monitored every other day. Tumor volumes are measured every 3 to 4 days. Tumor volumes are calculated using the formula: 0.5 × (larger diameter) × (small diameter)2.

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

    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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8076 mL 14.0382 mL 28.0765 mL 70.1912 mL
    5 mM 0.5615 mL 2.8076 mL 5.6153 mL 14.0382 mL
    10 mM 0.2808 mL 1.4038 mL 2.8076 mL 7.0191 mL
    15 mM 0.1872 mL 0.9359 mL 1.8718 mL 4.6794 mL
    20 mM 0.1404 mL 0.7019 mL 1.4038 mL 3.5096 mL
    25 mM 0.1123 mL 0.5615 mL 1.1231 mL 2.8076 mL
    30 mM 0.0936 mL 0.4679 mL 0.9359 mL 2.3397 mL
    40 mM 0.0702 mL 0.3510 mL 0.7019 mL 1.7548 mL
    50 mM 0.0562 mL 0.2808 mL 0.5615 mL 1.4038 mL
    60 mM 0.0468 mL 0.2340 mL 0.4679 mL 1.1699 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:
    GSK 3 Inhibitor IX
    目录号:
    HY-10580
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