1. Metabolic Enzyme/Protease
  2. E1/E2/E3 Enzyme
  3. PYZD-4409

PYZD-4409 是 ubiquitin-activating enzyme UBA1 的特异性抑制剂,其 IC50 值为 20 μM。PYZD-4409 能诱导恶性细胞死亡,并优先抑制原发性急性髓性白血病细胞的生长。

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PYZD-4409 Chemical Structure

PYZD-4409 Chemical Structure

CAS No. : 423148-78-1

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

WB

    PYZD-4409 purchased from MCE. Usage Cited in: Mol Cell Biol. 2018 Jul 16;38(15). pii: e00024-18.  [Abstract]

    Western blotting assays demonstrate that treatment of 20 μM PYR-41 or 20 μM PYZD-4409 inhibits ubiquitination and CD133 secretion. Hsp90 and β-actin are used as loading controls.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells[1].

    IC50 & Target

    IC50: 20 μM (ubiquitin-activating enzyme UBA1)[1]

    体外研究
    (In Vitro)

    PYZD-4409 (10-40 μM; 72 hours; myeloma, leukemia, and solid tumor cell lines, primary AML cells and normal hematopoietic cells) induces cell death with a LD50 less than 10 μM in 5 of 8 leukemia and myeloma cell lines. In contrast, solid tumor cell lines were less sensitive with an LD50 of approximately 15 to 20 μM. PYZD-4409 is preferentially cytotoxic to malignant cells over normal hematopoietic cells[1].
    PYZD-4409 (50 μM; 4 hours; K562 leukemia cells) treatment blocks the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc34[1].
    PYZD-4409 (0-25 μM; 24 hours; K562 leukemia cells) significantly increases both mRNA and protein levels of Grp78 and Hsp70. In addition, PYZD-4409 increases levels of phospho-JNK and phospho-p38 mitogen-activated protein kinase, which have also been linked to ER stress and the unfolded protein response[1].

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

    Cell Cytotoxicity Assay[1]

    Cell Line: Myeloma, leukemia, and solid tumor cell lines, primary AML cells and normal hematopoietic cells
    Concentration: 10 μM, 20 μM, 30 μM, 40 μM
    Incubation Time: 72 hours
    Result: Induced cell death with a LD50 less than 10 μM in 5 of 8 leukemia and myeloma cell lines. In contrast, solid tumor cell lines were less sensitive with an LD50 of approximately 15 to 20 μM.

    Western Blot Analysis[1]

    Cell Line: K562 leukemia cells
    Concentration: 50 μM
    Incubation Time: 4 hours
    Result: Blocked the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc34.

    RT-PCR[1]

    Cell Line: K562 cells
    Concentration: 0 μM, 10 μM, 25 μM
    Incubation Time: 24 hours
    Result: Significantly increased both mRNA and protein levels of Grp78 and Hsp70.
    体内研究
    (In Vivo)

    PYZD-4409 (10 mg/kg; intraperitoneal injection; daily on alternate days; for 16 days; male severe combined immunodeficient mice) decreases tumor weight and volume without untoward toxicity[1].

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

    Animal Model: Male severe combined immunodeficient (SCID) mice with MDAY-D2 murine leukemia cells[1]
    Dosage: 10 mg/kg
    Administration: Intraperitoneal injection; daily on alternate days; for 16 days
    Result: Delayed tumor growth and decreased tumor weight without untoward toxicity.
    分子量

    351.67

    Formula

    C14H7ClFN3O5

    CAS 号
    性状

    固体

    颜色

    Light brown to black

    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 : ≥ 35 mg/mL (99.53 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 2.8436 mL 14.2179 mL 28.4357 mL
    5 mM 0.5687 mL 2.8436 mL 5.6872 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.11 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。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    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
    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
    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 2.8436 mL 14.2179 mL 28.4357 mL 71.0894 mL
    5 mM 0.5687 mL 2.8436 mL 5.6871 mL 14.2179 mL
    10 mM 0.2844 mL 1.4218 mL 2.8436 mL 7.1089 mL
    15 mM 0.1896 mL 0.9479 mL 1.8957 mL 4.7393 mL
    20 mM 0.1422 mL 0.7109 mL 1.4218 mL 3.5545 mL
    25 mM 0.1137 mL 0.5687 mL 1.1374 mL 2.8436 mL
    30 mM 0.0948 mL 0.4739 mL 0.9479 mL 2.3696 mL
    40 mM 0.0711 mL 0.3554 mL 0.7109 mL 1.7772 mL
    50 mM 0.0569 mL 0.2844 mL 0.5687 mL 1.4218 mL
    60 mM 0.0474 mL 0.2370 mL 0.4739 mL 1.1848 mL
    80 mM 0.0355 mL 0.1777 mL 0.3554 mL 0.8886 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:
    PYZD-4409
    目录号:
    HY-13297
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