Chemical Structure : MS351
CAS No.:
439127-06-7
MS351
(MS-351)
Catalog No.: PC-26724Not For Human Use, Lab Use Only.
MS351 (MS-351) is a specific small molecule antagonist of chromobox 7 (CBX7) chromodomain (CBX7ChD) with Kd of approximately 500 uM by NMR titration, disrupts H3K27me3-mediated CBX7 binding to target genes in chromatin.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
MS351 (MS-351) is a specific small molecule antagonist of chromobox 7 (CBX7) chromodomain (CBX7ChD) with Kd of approximately 500 uM by NMR titration, disrupts H3K27me3-mediated CBX7 binding to target genes in chromatin.
MS351 does not bind ChDs from other CBX proteins including CBX1/3/5 (HP1β/γ/α) and CBX2/4/6/8 ,or the bromodomains of BRD4.
MS351 has the unique ability to bind and form a ternary complex with CBX7ChD and a predicated hairpin RNA derived from ANRIL with Kd of 23.8 uM.
MS351 effectively induces transcriptional derepression of p16INK4a in human prostate cancer PC3 cells in a dose-dependent manner at 1-5 uM.
MS351 (0.5 uM) effectively induced derepression of other CBX7 target genes including Hoxd3 and Noggin in mouse ES cells.er CBX7 target genes including Hoxd3 and Noggin in mouse ES cells
Physicochemical Properties
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M.Wt
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426.34
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Formula
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C23H21Cl2N3O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(3,4-dichlorophenyl)-2-(2-imino-3-(2-methylbenzyl)-2,3-dihydro-1H-benzo[d]imidazol-1-yl)ethan-1-ol
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References
1. Chunyan Ren, et al. ACS Med Chem Lett. 2016 Feb 29;7(6):601-5.
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