產(chǎn)品目錄

規(guī)格	5mg 10mg 50mg 100mg
CAS	1609402-14-3
別名	N/A
化學(xué)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)
儲(chǔ)存條件	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 All other available size: ship with RT , or blue ice upon request

產(chǎn)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.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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