CADD522,199735-88-1

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CADD522

CAS No. : 199735-88-1

MCE 国际站：CADD522

产品活性：CADD522 是一种 RUNX2-DNA 结合抑制剂 (下调 RUNX2 介导的下游靶基因的转录)，其 IC₅₀ 值为 10 nM。CADD522 还可通过增加线粒体驱动的细胞 ROS 水平发挥其抗肿瘤活性。CADD522 能抑制体内原发肿瘤的生长和免疫受损小鼠肺部肿瘤细胞的实验性转移，可用于癌症的研究。

研究领域：Immunology/Inflammation  |  NF-κB  |  Metabolic Enzyme/Protease

作用靶点：Reactive Oxygen Species

In Vitro: CADD522 (0-100 μM; 24-72 h) exhibits a strong inhibitory effect on BC cell growth and survival.
CADD522 (50 μM; 72 h) shows anti-proliferative effect by inducing cell cycle arrest (G1 phase).
CADD522 (50 μM; 8 days) inhibits tumorsphere formation and (50 μM; 24 h) in vitro invasion of BC cells (without cellular toxicity).
CADD522 (2, 10, 25, 50, 100 μM; 48 h) inhibits RUNX2 transcriptional activity by inhibiting RUNX2-DNA binding in T47D-RUNX2 and T47D-Empty cells.
CADD522 (50 μM; 72 h) upregulates RUNX2 levels through increased RUNX2 stability in cells.
CADD522 (50 μM; 6 or 24 h) increases ROS generation of mitochondrial in MCF7 and MDA-468 cells.
CADD522 (0-2000 nM, 30 min) inhibits mitochondrial ATP synthase activity in MDA-231 and MDA-468 cells.

In Vivo: CADD522 (1, 5 and 20 mg/kg; i.p.; twice a week for 45 days) delays the onset of the tumors and suppresses tumor growth in mice.
CADD522 (10 mg/kg; i.p.; twice a week for 11 days) suppresses tumor metastasis and inhibits expression of Ki-67 in mice.

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