1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Autophagy Apoptosis
  2. HSP Autophagy Apoptosis
  3. HA15

HA15 是一种高效特异性的内质网伴侣蛋白 BiP/GRP78/HSPA5 抑制剂,可抑制 BiP 的 ATP 酶活性,具有抗肿瘤活性。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

HA15 Chemical Structure

HA15 Chemical Structure

CAS No. : 1609402-14-3

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥847
In-stock
1 mg ¥350
In-stock
5 mg ¥770
In-stock
10 mg ¥1100
In-stock
50 mg ¥3500
In-stock
100 mg ¥5413
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

注册 MCE会员完成审核
即刻享有 积分商城 300 专属积分

Top Publications Citing Use of Products

    HA15 purchased from MCE. Usage Cited in: Sci Rep. 2020 Jun 30;10(1):10604.  [Abstract]

    HA15, a GRP78 inhibitor, to inhibit GRP78, and finds that inhibition of GRP78 abolished the downregulation of Col1 and α-SMA in response to UCHL1 siRNA in CFs with TGF-β1 stimulation.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity[1].

    IC50 & Target

    BiP/GRP78/HSPA5[1]

    体外研究
    (In Vitro)

    HA15 (10 μM; 1-24 hours) induces an early endoplasmic reticulum stress (ER Stress)[1].
    ? HA15 (0-10μM; 24 hours) decreases melanoma cell viability in a dose-dependent manner compared with control conditions (DMSO), with an IC50 of 1-2.5 μM in? A375 cells[1].
    ? HA15 (1-10 μM; 24 hours) induces apoptosis in A375 cells[1].
    ? HA15 (1-24 μM; 24 hours) induces autophagy[1].
    ? HA15 (10 μM; 48 hours) has high efficiency in inducing cell death and ER stress in BRAF-inhibitor-resistant melanoma cells. And HA15 inhibits tumor growth through autophagic and apoptotic mechanisms initiated by ER stress[1].
    ? No deleterious effects on the viability of normal human melanocytes or human fibroblasts were observed with low or high doses of HA15[1].

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

    Cell Viability Assay[1]

    Cell Line: A375 cells
    Concentration: 1 μM,2.5 μM,5 μM,7.5 μM,10 μM
    Incubation Time: 24 hours
    Result: Decreased melanoma cell viability in a dose-dependent manner compared with control conditions (DMSO) in A375 cells.

    Apoptosis Analysis[1]

    Cell Line: A375 cells
    Concentration: 1 μM, 5 μM, 10 μM
    Incubation Time: 24 hours
    Result: Induces apoptosis.

    Cell Autophagy Assay[1]

    Cell Line: A375 cells
    Concentration: 1 μM, 4 μM, 10 μM, 24 μM
    Incubation Time: 24 hours
    Result: Increased LC3B-II expression after 1 hour and persisted after 24 hours, enhanced the expression level of Beclin 1, clearly be indicated that induces autophagy.

    Western Blot Analysis[1]

    Cell Line: A375 cells
    Concentration: 10 μM
    Incubation Time: 1 hour, 4 hours, 10 hours, 24 hours
    Result: Exhibited a rapid induction within 1 hour of the ER stress markers (phosphorylation of PERK and elF2α and a weak increase in ATF4 and CHOP expression)
    体内研究
    (In Vivo)

    HA15 (0.7 mg/mouse/day; i.h.; over 2 weeks) inhibits melanoma tumor development in mice, induces no apparent toxicity and no change in their behavior, body mass, or liver mass, suggesting an absence of hepatomegaly[1].
    ? HA15 (0.7 mg/mouse; i.p.; 5 days/week) suppresses MPM tumor growth in vivo[3].

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

    Animal Model: 6-weeks female BALB/c nu/nu (nude) mice with A375 melanoma cells xenograft[1]
    Dosage: 0.7 mg/mouse/day
    Administration: Subcutaneous injection; over a period of 2 weeks
    Result: Attenuated the development of tumors.
    Animal Model: Mouse, NSG (NOD-scid IL2Rγnull)[3]
    Dosage: 0.7 mg/mouse
    Administration: Intraperitoneal injection, 5 days/week, for 5 weeks
    Result: Suppressed MPM tumor growth.
    分子量

    466.58

    Formula

    C23H22N4O3S2

    CAS 号
    性状

    固体

    颜色

    Light yellow to green 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 : ≥ 50 mg/mL (107.16 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 2.1433 mL 10.7163 mL 21.4326 mL
    5 mM 0.4287 mL 2.1433 mL 4.2865 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 (5.36 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

    纯度: 99.62%

    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 2.1433 mL 10.7163 mL 21.4326 mL 53.5814 mL
    5 mM 0.4287 mL 2.1433 mL 4.2865 mL 10.7163 mL
    10 mM 0.2143 mL 1.0716 mL 2.1433 mL 5.3581 mL
    15 mM 0.1429 mL 0.7144 mL 1.4288 mL 3.5721 mL
    20 mM 0.1072 mL 0.5358 mL 1.0716 mL 2.6791 mL
    25 mM 0.0857 mL 0.4287 mL 0.8573 mL 2.1433 mL
    30 mM 0.0714 mL 0.3572 mL 0.7144 mL 1.7860 mL
    40 mM 0.0536 mL 0.2679 mL 0.5358 mL 1.3395 mL
    50 mM 0.0429 mL 0.2143 mL 0.4287 mL 1.0716 mL
    60 mM 0.0357 mL 0.1786 mL 0.3572 mL 0.8930 mL
    80 mM 0.0268 mL 0.1340 mL 0.2679 mL 0.6698 mL
    100 mM 0.0214 mL 0.1072 mL 0.2143 mL 0.5358 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.

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称:

     

    * 需求量:

    * 客户姓名:

     

    * Email:

    * 电话:

     

    * 公司或机构名称:

       留言给我们:

    Bulk Inquiry

    Inquiry Information

    产品名称:
    HA15
    目录号:
    HY-100437
    需求量: