- Cat. No.
- A12948
UNC1215
UNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity.
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Epigenetic reader domain inhibitors, mostly bromodomain inhibitors, block recognition of acetylated histone lysines. Structural work on a histone acetyltransferase bromodomain first showed that this module binds acetylated lysine. Proteins of the bromodomain and extra-terminal (BET) family, such as bromodomain-containing protein 4 (BRD4), link histone acetylation to gene transcription. The thienodiazepine (+)-JQ1 was described in 2010 as a selective BET inhibitor that displaces BRD4 from chromatin. PFI-1, GSK1324726A and CPI-203 provide further BET inhibitor chemotypes for comparative studies. Other entries reach beyond BET binding, such as SGC-CBP30 for a non-BET bromodomain and the BRD4-degrading compound ARV-825.
UNC1215 is a potent, selective antagonist of L3MBTL3 with cellular activity.
UNC669 is a small-molecule antagonist of methyl-lysine (KMe) reader protein with selectivity for L3MBTL1 and L3MBTL3 (IC50 of 4.2μM and 3.1μM respectively)
MZ1 is a potent inducer of reversible, long-lasting and selective removal of BRD4 over BRD2 and BRD3.
TTK21 is a CBP/p300 histone acetyltransferase activator.
653-47 hydrochloride is a potentiator that significantly enhances the CREB (cAMP-response element-binding protein) inhibitory activity of 666-15. It also functions as a very weak CREB inhibitor on its own, with an IC₅₀ of 26.3 μM.
UNC3866 TFA is a selective antagonist of the CBX7-H3 interaction, exhibiting a potency with an IC50 value of 66±1.2 nM as determined by AlphaScreen assays. This compound shows over 100-fold selectivity for CBX7 compared to other members of the methyl-lysine reader panel. UNC3866 TFA is valuable for research applications focused on elucidating the role of CBX7 in epigenetic regulation and potential therapeutic strategies targeting this pathway.
UNC4976 is a positive allosteric modulator of the CBX7 chromodomain, targeting nucleic acid binding. It functions by antagonizing the H3K27me3-specific recruitment of CBX7 to target genes while enhancing non-specific binding to DNA and RNA. This compound is valuable for research focused on chromatin regulation and the epigenetic mechanisms involved in gene expression.
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C-82 is a selective antagonist of CBP/β-catenin interaction, designed to inhibit the binding of β-catenin to CBP while promoting its association with p300. This compound effectively modulates the Wnt signaling pathway, making it a valuable tool for research in cancer biology and developmental processes. C-82 serves as an important reagent for studies investigating the role of β-catenin in transcriptional regulation and related disease mechanisms.
BRD4 Inhibitor-37 is a selective antagonist of the Epigenetic Reader Domain BRD4, demonstrating significant anticancer activity. With an IC50 ranging from 0.05-0.1 μM in binding assays and a GI50 of 0.1-0.3 μM in cellular models, this compound effectively impedes the c-Myc signaling pathway, a critical downstream target of BRD4. Its selectivity across multiple bromodomain proteins positions BRD4 Inhibitor-37 as an important tool for investigating BET protein functions in cancer research and therapeutic development.