MS37452|cas 423748-02-1|DC Chemicals

Cas No.:	423748-02-1
Chemical Name:	MS37452
Synonyms:	MS37452
SMILES:	CC1C=CC=C(OCC(N2CCN(C(C3=CC=CC(OC)=C3OC)=O)CC2)=O)C=1
Formula:	C₂₂H₂₆N₂O₅
M.Wt:	398.452246189117
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	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[1].
Target:	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]. RT-PCR[1] 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.
References:	[1]. Ren C, et al. Small-molecule modulators of methyl-lysine binding for the CBX7 chromodomain. Chem Biol. 2015;22(2):161-168.

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