化学性质:
规格 | 5mg 10mg 50mg 100mg |
CAS | 1609402-14-3 |
别名 | N/A |
化学名 | N/A |
分子式 | C23H22N4O3S2 |
分子量 | 466.58 |
溶解度 | DMSO : ≥ 50 mg/mL (107.16 mM);H2O : < 0.1 mg/mL (insoluble) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
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[1].
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].
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].
References:
[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.
特别提醒:
1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。
2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。
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