p-37

TGP-377 421 (Targapre-miR-377 421) is a potent dual inhibitor that binds to and inhibits miR-377 and miR-421 at their functional sites.

CEP-37440 is an effective and specific Dual FAK ALK inhibitor with IC50s of 120 nM(ALK cellular in 75% human plasma) and 2.3 nM (FAK).

CP 376395 hydrochloride is a potent and selective CRF-RI receptor antagonist.

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)

FD223 is a potent, selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor with a marked affinity (IC50=1 nM), demonstrating notable selectivity against other isoforms (IC50s: α=51 nM, β=29 nM, γ=37 nM). This compound effectively suppresses the proliferation of acute myeloid leukemia (AML) cell lines by inhibiting p-AKT Ser473, thereby inducing G1 phase cell cycle arrest. FD223 holds promise for leukemia research, particularly in AML[1].

P-gp modulator 3 (Compound 37) is a potent, competitive metabotropic P-glycoprotein (P-gp) modulator.

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.

HDAC6-IN-37 (compound W5), an HDAC6 inhibitor, exhibits neuroprotective properties. It effectively restores the morphology of hippocampal neurons and diminishes the expression of Aβ, Tau, and p-Tau proteins in the hippocampus of AD rats. Additionally, it prevents the formation of senile plaques and neurofibrillary tangles. Consequently, HDAC6-IN-37 ameliorates the symptoms in the Aβ Cu 2+ -induced AD rat model, regulates oxidative stress, and restores balance to neurotransmitter levels in brain tissue [1].