Selective protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 1.8 μM). Exhibits five-fold selectivity for PRMT1 over PRMT6 and >250-fold selectivity over PRMT3 and CARM1.
11(Z),14(Z),17(Z)-Eicosatrienoic acid methyl ester is the ester derivative of 11(Z),14(Z),17(Z)-eicosatrienoic acid, identified within lipid-producing microalgae Nannochloropsis, as well as in diesel-contaminated soils and residential wastewater.
12(Z),15(Z)-Heneicosadienoic acid, an ω-6 very long-chain polyunsaturated fatty acid, serves as a positional isomer of heneicosadienoic acid, which is scarcely found in living organisms.
CC214-2 is a potent dual inhibitor of mTORC1 and mTORC2, known for its ability to impede autophagy by modulating mammalian target of rapamycin (mTOR) signaling. With this capacity, CC214-2 shows promise in shortening the duration of tuberculosis (TB) [1].
BSc2118 is a potent proteasome inhibitor. BSc2118 shows significant antimyeloma activity and may be considered as a promising agent in cancer drug development. BSc2118 is also a promising new candidate for stroke therapy, which may in addition alleviate recombinant tissue-plasminogen activator-induced brain toxicity.
53BP1-binding protein 1 (53BP1) engages with dimethylated lysine 20 on histone 4 (H4K20me2) through its tandem tudor domains within a homodimer configuration, crucial for the DNA damage response. UNC2170, a micromolar 53BP1 ligand, selectively interacts with this site, demonstrating at least 17-fold preference for 53BP1 over similar proteins. This interaction occurs in a pocket formed by the 53BP1's tudor domains. Moreover, UNC2170 acts as an antagonist to 53BP1 in cellular lysates, effectively inhibiting class switch recombination, a process dependent on the functional 53BP1 tudor domain, thus confirming its cellular activity.