MS37452MS37452
MedChemExpress (MCE)
HY-119344
423748-02-1
99.81%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
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.
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[1]. MS37452 (250 μM
2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus[1]. MS37452 (200 µM
5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment[2]. MS37452 (200 µM
5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy[2].
CBX7[1] 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[1]. MS37452 (250 μM
2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus[1]. MS37452 (200 µM
5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment[2]. MS37452 (200 µM
5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> MS37452 Related Antibodies RT-PCR[1] Cell Line: PC3 cells
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[1]. Ren C, et al. Small-molecule modulators of methyl-lysine binding for the CBX7 chromodomain. Chem Biol. 2015
22(2):161-168. [Content Brief]
[2]. Connelly KE, et al. CBX Chromodomain Inhibition Enhances Chemotherapy Response in Glioblastoma Multiforme. Yale J Biol Med. 2016
89(4):431-440.