产品
编 号:F192406
分子式:C23H22N4O3S2
分子量:466.58
产品类型
结构图
CAS No: 1609402-14-3
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产品详情
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.
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.