产品
编 号:F355078
分子式:C22H26N2O5
分子量:398.45
产品类型
结构图
CAS No: 423748-02-1
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产品详情
生物活性:
MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells.
体外研究:
MS37452 (125-500 μM; 12 hours) significantly increases INK4A/ARF transcript levels up to 25% and 60% for 250 μM and 500 μM, respectively, as compared to the DMSO control.MS37452 (250 μM; 2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus.MS37452 (200 μM; 5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment.MS37452 (200 μM; 5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy.