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

HA15 

目录号: HY-100437 纯度: 99.62%
产品使用指南

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。

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HA15 Chemical Structure

HA15 Chemical Structure

CAS No. : 1609402-14-3

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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
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥847
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5 mg ¥770
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10 mg ¥1100
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50 mg ¥3500
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100 mg ¥6000
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500 mg   询价  

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Top Publications Citing Use of Products

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

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

    DMSO : ≥ 50 mg/mL (107.16 mM)

    * "≥" 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
    10 mM 0.2143 mL 1.0716 mL 2.1433 mL
    *

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

    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

    • 1.

      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); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.36 mM,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 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献
    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    HA15
    目录号:
    HY-100437
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