MS37452

MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3 , with a K d 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 In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell Line: PC3 cells Concentration: 125-500 μM Incubation Time: 12 hours Result: Up-regulated INK4A/ARF expression up to 25% and 60% for 250 μM and 500 μM, respectively. Cell Viability AssayCell Line: Glioblastoma multiforme (GBM) U118MG cells Concentration: PRT4165 40 µM, PTC209 200 nM, DZnep 25 µM, GSK343 400 nM, MS37452 200 µM, Doxorubicin 200 nM, temozolomide 50 µM, SAHA 1 µM Incubation Time: 5 days Result: Identified several combinations that resulted in consistently decreased cell viability compared to DMSO treated and single drug treatment: SAHA/TMZ and MS37452/doxorubicin. Form:Solid IC50& Target:CBX7

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