S81369 |
HA15 |
| 源叶(MedMol) | 99% |
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- 产品描述： HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity
- 靶点： BiP/GRP78/HSPA5
- 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. 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 ind
- 体内研究： 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. 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.
- 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.
- 溶解性： soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.143 ml 10.716 ml 21.433 ml 5 mM 0.429 ml 2.143 ml 4.287 ml 10 mM 0.214 ml 1.072 ml 2.143 ml 50 mM 0.043 ml 0.214 ml 0.429 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
