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.
性状
Solid
IC50 & Target[1][2]
CBX7
体外研究(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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
RT-PCR
Cell 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.
Identified several combinations that resulted in consistently decreased cell viability compared to DMSO treated and single drug treatment: SAHA/TMZ and MS37452/doxorubicin.