HA15

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HA15  纯度: 99.62%

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。

HA15

HA15 Chemical Structure

CAS No. : 1609402-14-3

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 In-stock
5 mg ￥770 In-stock
10 mg ￥1100 In-stock
50 mg ￥3500 In-stock
100 mg ￥6000 In-stock
200 mg   询价  
500 mg   询价  

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HA15 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Anti-Aging Compound Library
  • Endoplasmic Reticulum Stress Compound Library
  • Cytoskeleton Compound Library

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].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 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

1609402-14-3
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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Cerezo M et al. Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance. Cancer Cell. 2016 Jun 13;29(6):805-19.

    [2]. Ruggiero C, et al. The GRP78/BiP inhibitor HA15 synergizes with mitotane action against adrenocortical carcinoma cells through convergent activation of ER stress pathways. Mol Cell Endocrinol. 2018 Oct 15;474:57-64.

    [3]. Duo Xu, et al. Endoplasmic Reticulum Stress Signaling as a Therapeutic Target in Malignant Pleural Mesothelioma. Cancers (Basel). 2019 Oct; 11(10): 1502.

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