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编 号:F745332
分子式:C24H42N6O5
分子量:494.63
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生物活性:
OHM1 is an analog of HIF1α CTAD that inhibits its binding with p300/CBP. OHM1 targets CH1 domain with an affinity of 0.53 μM.

体内研究:
OHM1 (15 mg/kg; i.p.; every other day for 15 injections) 降低小鼠 MDA-MB-231 肿瘤体积。Animal Model:BALB/c mice, MDA-MB-231 xenograft model
Dosage:15 mg/kg
Administration:Intraperitoneal injection, every other day for 15 injections
Result:Reduced the median tumor volume by roughly 50% compared with the untreated group. Did not cause measurable changes in animal body weight or other signs of toxicity in tumor-bearing animals, nor increased the metastasis rate.

体外研究:
OHM1 (1-20 μM; 24 h) 导致 HIF 启动子活性呈剂量依赖性降低,并在 20 μM 使 MDA-MB-231 细胞在低氧条件下的 HIF1α 转录活性降低至常氧条件下.OHM1 下调缺氧诱导基因表达。OHM1 (10 μM) 下调了 A549 非小细胞肺癌细胞系中与血管生成、凋亡、细胞增殖和侵袭相关的多个基因,以及几种癌症特异性标记物。
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