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HA15

CAS No. : 1609402-14-3

MCE 国际站：HA15

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Metabolic Enzyme/Protease  |  Autophagy  |  Apoptosis

作用靶点：HSP  |  Autophagy  |  Apoptosis

In Vitro: 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.

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.

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