a-128

elomycin is a cyclic depsipeptide antibiotic with activity against Gram-positive bacteria.

TOK-8801 is a synthetic dihydroimidazole thiazole carboxamide with immunomodulatory activity that eliminates the stimulatory effects of antibody production by removing T cells.128-63-63-5

Lecimibide (DuP 128) is a potent and selective inhibitor of acyl coenzyme A:cholesterol acyltransferase (ACAT), useful for studying high-lipid-related diseases.

KB-5492 FA is a selective sigma receptor inhibitor with antiulcerogenic effects.128-52-56-8

Pobilukast (SKF 104353) is a selective cysteinyl leukotriene receptor antagonist that blocks phosphatidylinositol metabolism and leukotriene D-induced thromboxane synthesis, and can be used to study limiting myocardial damage in excessively myocardial reperfusion-injured (MI R) rats.128-63-53-4

PARP-2-IN-3 is used as a potent PARP-2 inhibitor (IC50=0.07 μM) with anti-tumor activity that induces apoptosis and necrosis in cancer cells, and can be used for the study of breast cancer.128-52-56-8

VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of the mGlu4 receptor with an EC50 of 240 nM for human receptors and 110 nM for rat receptors. It exhibits weak activity at mGlu5 and mGlu8 receptors and is inactive at mGlu1, mGlu2, mGlu3, mGlu6, and mGlu7 receptors. The compound can penetrate the CNS.

Thienopyridone is a potent and selective inhibitor of phosphatase of regenerating liver (PRL) phosphatase [IC50 values of 173 nM for PRL-1, 277 nM for PRL-2, and 128 nM for PRL-3], and induces p130Cas cleavage and apoptosis with anticancer effects.

EGFR-IN-128 (compound 28) is a potent and selective molecule targeting wild-type EGFREx20Ins, demonstrating therapeutic efficacy across various human xenograft models and capable of penetrating the blood-brain barrier in preclinical species.

CYP51-IN-2 (compound 1b), a Fluconazole analog, serves as a potent antifungal agent. It exhibits activity against Gypseum and Candida Albicans that is 64 and 128 times higher, respectively, compared to Fluconazole.

MDA7 is a selective agonist of the cannabinoid receptor 2 (CB2), demonstrating an EC50 of 128 nM in human CB2 receptors and 67.4 nM in rat CB2 receptors. The compound exhibits good affinity for CB2 receptors, with Ki values of 422 nM for humans and 238 nM for rats. In rat models, MDA7 shows analgesic activity.

PZ-128, a PAR1 antagonist, is used potentially for the treatment of thrombosis.

YKAs3003, a potent inhibitor of pathogenic KAS III, displays minimal inhibitory concentration (MIC) values in the range 128-256 microg/mL against various bacteria.

AD 128 is a bioactive chemical and therapeutic agent.

β-Defensin-1 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth ofB. adolescentis,L. acidophilus,B. breve,B. vulgatus,L. fermentum,B. longum, andS. thermophilusin an antimicrobial radial diffusion assay.2β-Defensin-1 also inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius, and of susceptibleM. tuberculosisH37Rv but not of resistantM. tuberculosisRM22 when used at a concentration of 128 μg/ml.3,4It blocks human and mouse Kv1.3 voltage-gated potassium channels (IC50s = 11.8 and 13.2 μM, respectively).5Overexpression of β-defensin-1 in the human oral squamous cell carcinoma (OSCC) cell lines HSC-3, UM-1, and SCC-9 increases migration and invasion but not proliferation.6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Schroeder, B.O., Ehmann, D., Precht, J.C., et al.Paneth cell α-defensin 6 (HD-6) is an antimicrobial peptideMucosal Immunol.8(3)661-671(2015) 3.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) 4.Fattorini, L., Gennaro, R., Zanetti, M., et al.In vitro activity of protegrin-1 and beta-defensin-1, alone and in combination with isoniazid, against Mycobacterium tuberculosisPeptides25(7)1075-1077(2004) 5.Feng, J., Xie, Z., Yang, W., et al.Human beta-defensin 1, a new animal toxin-like blocker of potassium channelToxicon113(2016) 6.Han, Q., Wang, R., Sun, C., et al.Human beta-defensin-1 suppresses tumor migration and invasion and is an independent predictor for survival of oral squamous cell carcinoma patientsPLoS One9(3)e91867(2014)

28-Acetylbetulin is a lupane triterpenoid and derivative of the cholesterol biosynthesis inhibitor betulin that has been found inM. chiapensisand has anti-inflammatory and anticancer activities.1,2It inhibits LPS-induced nitric oxide (NO) and prostaglandin E2production by 55.9 and 69.5%, respectively, in RAW 264.7 cells (IC50s = 4.7 and 1.7 μM, respectively).128-Acetylbetulin induces cytotoxicity in a variety of cancer cells, including A549, HT-29, and MCF-7 cells (IC50s = 14.37, 10.96, and 11.38 μM, respectively).2

Leoidin is a depsidone originally isolated from L. gangaleoides that has antibacterial and enzyme inhibitory activities.1,2,3 It is active against the bacteria E. faecalis, H. influenzae, M. catarrhalis, S. aureus, and S. pneumoniae (MICs = 8, 32, 1, 128, and 64 μg/ml, respectively).2 Leoidin inhibits phenylalanyl-tRNA synthetase (PheRS) isolated from P. aeruginosa (IC50 = 42 μM). It also inhibits organic anion-transporting polypeptide 1B1 (OATP1B1) and OATP1B3 with Ki values of 0.08 and 1.84 μM, respectively, in CHO cells expressing the human transporters.3

8-hydroxy Amoxapine is a metabolite of the tetracyclic antidepressant amoxapine .1,2 1.Johnson, S.M., Nygard, G., and Khalil, S.K.Isocratic liquid chromatographic method for the determination of amoxapine and its metabolitesJ. Pharm. Sci.73(5)696-699(1984) 2.Tasset, J.J., and Pesce, A.J.Amoxapine in human overdoseJ. Anal. Toxicol.8(3)124-128(1984)

(-)-Mycousnine is a microbial metabolite and derivative of usnic acid originally isolated fromM. nawaethat has antibacterial and antifungal activities.1,2It is active against the Gram-positive bacteriaB. subtilis,K. rhizophila, andS. aureus(MICs = 4, 8, and 4 g/ml, respectively) but not the Gram-negative bacteriaE. coli,S. typhimurium, andK. pneumoniae(MICs = >128 g/ml for all).2(-)-Mycousnine is also active against the fungiT. mentagrophytes,T. rubrum, andC. albicans(MICs = 25, 25, and 100 μg/ml, respectively).1 1.Sassa, T., and Igarashi, M.Structures of (-)-mycousnine, (+)-isomycousnine and (+)-oxymycousnine, new usnic acid derivatives from phytopathogenic Mycosphaerella nawaeAgric. BioI. Chem.54(9)2231-2237(1990) 2.Lee, J., Lee, J., Kim, G.J., et al.Mycousfurans A and B, antibacterial usnic acid congeners from the fungus Mycosphaerella sp., isolated from a marine sedimentMar. Drugs17(7)422(2019)

A-39183A is an active component of the A-39183 antibiotic complex produced by aerobic fermentation of Streptomyces NRRL 12049. It has activity against penicillin-resistant S. aureus 3055 and S. faecalis X66 (MICs = 32 and 32 μg/ml, respectively) and a variety of Gram-positive and Gram-negative anaerobic bacteria (MICs = 16-128 μg/ml) in an agar dilution assay.

Antibacterial agent 50 (example 47) is a compound exhibiting antibacterial activity with minimum inhibitory concentration (MIC) values of 32, 64, and 128 mcg mL against E. coli strains NCTC 13351, M 50, and 7 MP, respectively [WO2013030733A1].

KSC-34 is a covalent modifier of protein disulfide isomerase A1 (PDIA1).KSC-34 is a selective inhibitor targeting the a-site of PDIA1.It inhibits PDIA1 reductase activity in a time-dependent manner and is used to study diseases caused by abnormalities in amyloid.128-63-63-5

Bromodomain inhibitor-10 (compound 128) is a highly potent bromodomain activity inhibitor, exhibiting strong binding affinity with Kd values of 15.0 nM and 2500 nM for BRD4-1 and BRD4-2, respectively. It also effectively inhibits the production of IL12p40 [1].

ATP Synthase Inhibitor 2, a compound targeting Pseudomonas aeruginosa (PA) ATP synthase with an IC50 of 10 μg mL, fully inhibits the ATP synthesis activity of PA at a concentration of 128 μg mL [1].