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SKLB325

CAS No. :

MCE 站：SKLB325

产品活性：SKLB325 是一种 JMJD6 抑制剂，其结合亲和力 (K_D) 值为 0.755 μM，IC₅₀ 值为 0.7797 μM。SKLB325 在体内外对卵巢癌具有抗肿瘤作用。SKLB325 诱导细胞凋亡 (apoptosis)。SKLB325 在肾细胞癌 (RCC) 中表现出显着的抗肿瘤功效。

研究领域：Epigenetics

作用靶点：Histone Demethylase

In Vitro: SKLB325 suppresses ovarian cancer growth through inhibition of proliferation ａnd induction of apoptosis ａnd cell death, ａnd inhibiting angiogenesis may play a significant role in inhibiting tumor growth.
SKLB325 (0.25-16μM; for 24-72h) has significant inhibitory effects on the in vitro proliferation of ovarian cancer cells. Furthermore, the most effective concentration at which JMJD6 inhibited SKOV3 cell growth is 4μM, ａnd the optimal duration of action is 72h.
SKLB325 upregulates the expression of p53 ａnd its downstream effectors at both the mRNA ａnd protein levels in vitro.

In Vivo: SKLB325 (10mg/kg) has antitumor activities in an intraperitoneal xenograft model. SKLB325 significantly prolongs the survival of tumor-bearing mice without obvious side effects. SKLB325 treatment protocols were effective in suppressing SKOV3, ES2, CP70, ａnd A2780s tumor growth in nude mice.

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