HA15|cas:1609402-14-3|西域试剂

HA15,99.62%

产品编号：Bellancom-100437| CAS NO：1609402-14-3| 分子式：C₂₃H₂₂N₄O₃S₂| 分子量：466.58

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货号	价格	库存与货期
Bellancom-100437	￥770.00	杭州北京（现货）
Bellancom-100437	￥1100.00	杭州北京（现货）
Bellancom-100437	￥3500.00	杭州北京（现货）
Bellancom-100437	￥6000.00	杭州北京（现货）

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HA15

产品介绍

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。

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.

体外研究

HA15 (10 μM; 1-24 hours) induces an early endoplasmic reticulum stress (ER Stress).
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.
HA15 (1-10 μM; 24 hours) induces apoptosis in A375 cells.
HA15 (1-24 μM; 24 hours) induces autophagy.
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.
No deleterious effects on the viability of normal human melanocytes or human fibroblasts were observed with low or high doses of HA15.

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

Cell Viability Assay

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

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

Cell Autophagy Assay

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

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.
HA15 (0.7 mg/mouse; i.p.; 5 days/week) suppresses MPM tumor growth in vivo.

西域 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
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)
Dosage:	0.7 mg/mouse
Administration:	Intraperitoneal injection, 5 days/week, for 5 weeks
Result:	Suppressed MPM tumor growth.

体内研究

西域 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
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)
Dosage:	0.7 mg/mouse
Administration:	Intraperitoneal injection, 5 days/week, for 5 weeks
Result:	Suppressed MPM tumor growth.

体内研究

西域 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
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)
Dosage:	0.7 mg/mouse
Administration:	Intraperitoneal injection, 5 days/week, for 5 weeks
Result:	Suppressed MPM tumor growth.

性状

Solid

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