2. Protein Tyrosine Kinase/RTK
  3. c-Kit
  4. ISCK03

ISCK03是特异性的 SCF/c-Kit 和 CD117 的抑制剂。ISCK03 在 10 μM 时显著抑制 c-Kit 磷酸化。

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ISCK03 Chemical Structure

ISCK03 Chemical Structure

CAS No. : 945526-43-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
5 mg ￥600
In-stock
10 mg ￥1000
In-stock
25 mg ￥2200
In-stock
50 mg ￥3350
In-stock
100 mg ￥4913
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

ISCK03 相关抗体

Top Publications Citing Use of Products

    ISCK03 purchased from MCE. Usage Cited in: Cell Cycle. 2020 Aug;19(16):2074-2080.  [Abstract]

    The expressions of p-JAK/JAK and p-STAT3/STAT3 are examined by Western blot assay. SCF induces up-regulation of p-JAK/JAK and p-STAT3/STAT3, but this effect is effectively counteracted by the SCF/c-kit inhibitor ISCK03.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    ISCK03 is a SCF/c-Kit and CD117-specific inhibitor. ISCK03 significantly inhibits c-Kit phosphorylation at 10 μM[1][2][3].

    体外研究
    (In Vitro)

    Pretreatment of 501mel cells with ISCK03 inhibits SCF-induced c-kit phosphorylation dose dependently. ISCK03 also inhibits p44/42 ERK mitogen-activated protein kinase (MAPK) phosphorylation, which is known to be involved in SCF/c-kit downstream signaling. However ISCK03 does not inhibit hepatocyte growth factor (HGF)-induced phosphorylation of p44/42 ERK proteins[1]. ISCK03, a tyrosine kinase inhibitor specific to KIT, prevents survival of CCDC26-KD cells under low-serum conditions. All treated cells exhibits sensitivity to ISCK03 in a dose-dependent manner. After ISCK03 treatment, the survival of KD cells is suppressed to the same level as that of non-KD cells. Conversely, ISCK03 treatment has limited effects on the growth of control K562 and KD clone 3–4 cells under high-serum concentration conditions[2].

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

    ISCK03 相关抗体:
    体内研究
    (In Vivo)

    Oral administration of ISCK03 induces the dose-dependent depigmentation of newly regrown hair, and this is reversed with cessation of ISCK03 treatment. The topical application of ISCK03 promotes the depigmentation of UV-induced hyperpigmented spots. Fontana-Masson staining analysis shows epidermal melanin is diminished in spots treated with ISCK03[1].

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

    355.45

    Formula

    C19H21N3O2S
    CAS 号
    性状

    固体

    颜色

    Off-white to light 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 : ≥ 38 mg/mL (106.91 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 2.8133 mL 14.0667 mL 28.1334 mL
    5 mM 0.5627 mL 2.8133 mL 5.6267 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

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.03 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.03 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    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

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.50%

    COA (192 KB) HNMR (255 KB) LCMS (257 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    ATP is dispensed into 384-well plates, chemical compounds (ISCK03: 2.5, 5, 10, 100 μM) are added by replicative plate, and recombinant human c-kit protein is added for the kinase reaction. Following a 45-min incubation at 37°C, the development reaction is carried out for 40 min at room temperature. After the reaction is stopped, the coumrain and fluorescein fluorescence-emission signals are detected[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    To determine any cytotoxic effects of ISCK03 on 501mel cells, MTT assays are performed with various doses of ISCK03 (1, 5, 10 μM). 501mel cells are cultured with SCF alone (50 ng/mL) or SCF with ISCK03 for 48 h[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: To induce the hair cycle, depilation of skin on the back of the female C57BL/6 mice is performed. Briefly, the hair is removed from anesthetized mice. The rat antimouse c-kit-neutralizing monoclonal antibody ACK2 is administered intraperitoneally (50 mg) every day. ISCK03 is administered orally once a day. On days 21–28, animals are sacrificed or analyzed for repigmentation of the newly regrown hair shaft. Skin is harvested and fixed in paraffin or frozen for immunohistochemical analyses[1].

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

    ISCK03 相关分类

    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 2.8133 mL 14.0667 mL 28.1334 mL 70.3334 mL
    5 mM 0.5627 mL 2.8133 mL 5.6267 mL 14.0667 mL
    10 mM 0.2813 mL 1.4067 mL 2.8133 mL 7.0333 mL
    15 mM 0.1876 mL 0.9378 mL 1.8756 mL 4.6889 mL
    20 mM 0.1407 mL 0.7033 mL 1.4067 mL 3.5167 mL
    25 mM 0.1125 mL 0.5627 mL 1.1253 mL 2.8133 mL
    30 mM 0.0938 mL 0.4689 mL 0.9378 mL 2.3444 mL
    40 mM 0.0703 mL 0.3517 mL 0.7033 mL 1.7583 mL
    50 mM 0.0563 mL 0.2813 mL 0.5627 mL 1.4067 mL
    60 mM 0.0469 mL 0.2344 mL 0.4689 mL 1.1722 mL
    80 mM 0.0352 mL 0.1758 mL 0.3517 mL 0.8792 mL
    100 mM 0.0281 mL 0.1407 mL 0.2813 mL 0.7033 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.

    Keywords:

    ISCK03945526-43-2ISCK 03ISCK-03c-KitSCFRCD117Inhibitorinhibitorinhibit

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