SML2408
UNC3866 trifluoroacetate salt
≥98% (HPLC)
Synonym(s):
N-[4-(1,1-Dimethylethyl)benzoyl]-L-phenylalanyl-L-alanyl-L-leucyl-N6,N6-diethyl-L-lysyl-L-Serine methyl ester trifluoroacetate
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About This Item
Empirical Formula (Hill Notation):
C43H66N6O8
Molecular Weight:
795.02
UNSPSC Code:
12352200
Recommended Products
Assay
≥98% (HPLC)
form
lyophilized powder (white)
color
white to off-white
shipped in
wet ice
storage temp.
−20°C
Biochem/physiol Actions
Antagonist of chromodomains CBX4/7 of Polycomb repressive complex 1
UNC3866 inhibits the CBX chromodomains of the Polycomb repressive complex 1 (PRC1), which is involved in transcriptional repression. UNC3866 selectively targets CBX4 and CBX7 most potently, with Kd values of ∼100 nM. The PRC1 chromodomains facilitate PRC1-mediated transcriptional repression by targeting the complex to Trimethyllysine 27 on histone 3 (H3K27me3). UNC3866 antagonizes the methyllysine (Kme) reading function, and has been shown to inhibit the PC3 prostate cancer cell proliferation associated with CBX7 overexpression.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Jacob I Stuckey et al.
Nature chemical biology, 12(3), 180-187 (2016-01-26)
We report the design and characterization of UNC3866, a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. Polycomb CBX proteins regulate gene expression by targeting Polycomb repressive complex 1 (PRC1) to
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