Novel Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitor

Novel anti-virulence agent, rescuing nematodes from a Staphylococcus aureus infection and preventing the formation of biofilm in a dose-dependent manner without interfering with bacterial viability

Novel fluorescent UnaG ligand, binding UnaG with high affinity (Kd = 3 nM) to induce a 2.5-fold fluorescence intensity enhancement and a 10 nm red shift

Novel nonhematotoxic DNA intercalating agent with potent antitumor activity, inducing apoptosis via inhibition of key proteins in the PI3K/Akt/mTOR signaling pathway

UNC0737 is a negative control of UNC0638 and the N-methyl analog of UNC0638. UNC0737 was designed to eliminate the hydrogen bond interaction seen in the G9a-UNC0224 cocrystal structure between Asp1083 of G9a and the secondary amino group at the 4-position of UNC0224's quinazoline ring3. UNC0737 was >300-fold less potent than UNC0638 in G9a and GLP biochemical assays. As expected, UNC0737 was a poor inhibitor of G9a (IC50 = 5,000 ± 200 nM (n = 2)) and GLP (IC50 > 10,000 nM (n = 2)) in the SAHH-coupled assays.

Biotinylated UNC0638, enabling chemiprecipitation of G9a from whole cell lysates

Novel MYC protein stablizer, increasing the abundance of endogenous MYC proteintargeting the receptor tyrosine kinases KIT and platelet-derived growth factor receptor α (PDGFRα)

Novel inhibitor of ROP18, inhibiting ROP18 within cells, and abrogating its effects on the host IRG pathway

Novel Peptide Inhibitor for Calcium and Integrin Binding Protein 1 (CIB1)

Negative control for UNC1666 which is a dual Mer and Flt-3 tyrosine kinase inhibitor

Orally Active Adenosine A 1 Receptor Agonist

Novel Ligand of EEDm acting as an allosteric inhibitor of PRC2

Novel allosteric inhibitor of PRC2 catalytic activity

Novel allosteric inhibitor of PRC2 catalytic activity

Novel selective activator of PRC2-EED-I363M, showing minimal effects on the activity of PRC2-WT

Novel selective activator of PRC2-EED-I363M, showing minimal effects on the activity of PRC2-WT

Novel inhibitor for histone methyllysine reader proteins (KmeRP), targeting CBX5 chromodomain

Novel inhibitor for histone methyllysine reader proteins (KmeRP), targeting CBX5 chromodomain

Novel peptidomimetic antagonist of the PHF1 Tudor domain, binding both PHF1 Tudor domain and the related protein PHF19

Novel inhibitor for histone methyllysine reader proteins (KmeRP), targeting CBX5 chromodomain

Novel potent and selective PAM of CBX8, blocking H3K27me3 binding and enhancing CBX8 affinity for nucleic acids, evicting PRC1 from H3K27me3 targets triggering DLBCL cell differentiation

Novel β-arrestin-biased D2 receptor (D2R) agonist