3 ll

LL-K9-3, a selective hydrophobic tagging technology (HyT)-based degrader, specifically targets the CDK9-cyclin T1 complex, displaying DC50 values of 589 nM for cyclin T1 and 662 nM for CDK9. This compound consists of the CDK9 inhibitor, SNS 032, linked to a hydrophobic tag via a glycol linker. Notably, LL-K9-3 does not affect the degradation of other CDKs (CDK1, 2, 4, 5, 6, and 7). Tested in 22RV1 cells, it effectively reduces androgen receptor (AR) and cMyc expression by inducing the selective and synchronous degradation of CDK9 and cyclin T1.

Citrullinated LL-37 3cit is a host defense peptide with notable immunomodulatory and antimicrobial properties, which exhibits direct antiviral activity against human rhinoviruses (HRV) [1].

SIBA (5'-Deoxy-5'-isobutylthioadenosine) is a synthetic analogue of SAH, acts as an inhibitor of S-adenosylmethionine-mediated transmethylation. SIBA can interfere with a variety of enzymatic activities in vitro, such as SAH hydrolase, methylthioadenosine phosphorylase and cAMP phosphodiesterase. SIBA reversibly blocks the multiplication of herpes simplex type 1 virus (HSV)

Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.

NH2-C5-PEG4-N3-L-Lysine-PEG3-N3 is a seven-unit cleavable polyethylene glycol (PEG) antibody-drug conjugate (ADC) linker used in ADC synthesis[1].

AT-9283 L-lactate is an inhibitor of aurora kinase.

N3-L-Lys(Mtt)-OH is a click chemistry reagent featuring an azido group. It efficiently introduces an azido functional group into the N-terminal position of amino acid structural units within peptide sequences.

N3-L-Lys(Fmoc)-OH is a click chemistry reagent containing an azide group, allowing it to undergo copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with molecules that possess an alkyne group. It can also participate in strain-promoted alkyne-azide cycloaddition reactions (SPAAC) with molecules featuring DBCO or BCN groups.

N3-L-Lys(Boc)-OH is a click chemistry reagent featuring an azide group that can undergo a copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing an alkyne group. Additionally, it can participate in strain-promoted azide-alkyne cycloaddition reactions (SPAAC) with molecules that contain DBCO or BCN groups.

N3-L-Leu-OH (BHA) is utilized as a reagent in click chemistry. Known for its potential in linking nucleic acids, lipids, proteins, and various other molecules, click chemistry is favored in numerous research areas due to its high yield, specificity, and simplicity. The compound features an Azide group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition reactions (CuAAC) with molecules containing Alkyne groups. Additionally, it can engage in strain-promoted azide-alkyne cycloaddition reactions (SPAAC) with molecules bearing DBCO or BCN groups.

5Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is also an inhibitor of VEGF-R2 with IC50 of 52 nM.

MG-115 (Z-LL-Nva-CHO) is a potent and reversible inhibitor of proteasome , with K i s of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis [1] [2] [3].

β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 10, and 40 μg/ml, respectively. β-Defensin-2 induces IL-31 production by human peripheral blood-derived mast cellsin vitrowhen used at a concentration of 10 μg/ml and by rat mast cellsin vivofollowing a 500 ng intradermal dose.4Expression of β-defensin-2 is increased in psoriatic skin and chronic wounds.5,6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 3.Niyonsaba, F., Ushio, H., Nakano, N., et al.Antimicrobial peptides human β-defensins stimulate epidermal keratinocyte migration, proliferation and production of proinflammatory cytokines and chemokinesJ. Invest. Dermatol.127(3)594-604(2007) 4.Niyonsaba, F., Ushio, H., Hara, M., et al.Antimicrobial peptides human β-defensins and cathelicidin LL-37 induce the secretion of a pruritogenic cytokine IL-31 by human mast cellsJ. Immunol.184(7)3526-3534(2010) 5.Huh, W.-K., Oono, T., Shirafuji, Y., et al.Dynamic alteration of human β-defensin 2 localization from cytoplasm to intercellular space in psoriatic skinJ. Mol. Med. (Berl.)80(10)678-684(2002) 6.Butmarc, J., Yufit, T., Carson, P., et al.Human β-defensin-2 expression is increased in chronic woundsWound Repair Regen.12(4)439-443(2004)

OP-145, a derivative of the antimicrobial peptide LL-37, is a synthetic antimicrobial peptide showing activity against E. coli, P. aeruginosa, C. albicans, and A. niger, with minimum inhibitory concentrations (MICs) of 2, 3, 6, and 18 µM, respectively. Utilizing poly(lactic-co-glycolic acid) (PLGA) microspheres loaded with OP-145 effectively prevents biofilm formation in a mouse model of bone infection, which is initiated by surgical femoral fracture and subsequent bacterial inoculation at the fracture site.

PD-1/PD-L1-IN 3 TFA inhibits the binding of human PD-1 to PD-Ll with an IC50 of 9 nM.