OX11 is a selective inhibitor of S. pneumoniae, P. aeruginosa, and E. coli bacterial strains[1].
Alisol F 24-acetate is a triterpene compound that can be isolated from the rhizomes of Alisma orientalis. Alisol F 24-acetate inhibits the secretion of HBV surface antigen HBsAg and HBeAg with IC50 values of 7.7 µM and 5.1 µM. Alisol F 24-acetate has proapoptotic activity and can be used for cancer research[1][2].
Tobevibart is an IgG1-lambda, anti-HBV (hepatitis B virus) surface envelope protein humanized monoclonal antibody. Tobevibart shows antiviral activity[1].
HCV-IN-44 (compound 28) is an HCV NS5B protein inhibitor that can effectively inhibit the replication of HCV virus. HCV-IN-44 can be used for the study of HCV infection[1].
HBV-IN-10 is an enantiomer of compound 6 (WO2021204258A1). Compound 6 is a hepatitis B surface antigen (HBsAg) inhibitor (0.001 μM< EC50 ≤0.05 μM). From patent WO2021204258A1, compound 6[1].
Nafcillin sodium monohydrate is a semi-synthetic antibiotic related to penicillin.Target: AntibacterialNafcillin sodium is a narrow-spectrum, beta-lactam antibiotic of the penicillin class. As a beta-lactamase-resistant penicillin, it is used to treat infections caused by Gram-positive bacteria, in particular, species of staphylococci that are resistant to other penicillins. Nafcillin is considered therapeutically equivalent to oxacillin, although its safety profile is somewhat different. Nafcillin was shown to reversibly inhibit beta-lactamase from Staphylococcus aureus PC1 with characteristics indicative of a type A inhibitor [Citri, Samuni & Zyk (1976) Proc. Natl. Acad. Sci. U.S.A. 73, 1048-1052]. At nafcillin concentrations above 80 mM, complete inactivation occurred within 200 s. Upon removal of the excess nafcillin the inhibited enzyme was re-activated completely, with a rate constant of 2.0 x 10(-3) s-1 (25 degrees C) [1, 2].
JAK2-IN-9 (Compound A8) is a selective JAK2 inhibitor (IC50: 5 nM). JAK2-IN-9 inhibits the phosphorylation of JAK2, STAT3, and STAT5. JAK2-IN-9 has metabolic stabilities. JAK2-IN-9 induces apoptosis. JAK2-IN-9 can be used for research of myeloproliferative neoplasms (MPNs)[1].
Methyl caffeate, an antimicrobial agent, shows moderate antimicrobial and prominent antimycobacterial activities. Methyl caffeate also exhibits α-glucosidase inhibition activity, oxidative stress inhibiting activity, anti-platelet activity, antiproliferative activity in cervix adenocarcinoma and anticancer activity in lung and leukmia cell lines[1].
ThrRS-IN-1 (Compound 30d) is a threonyl-tRNA synthetase (ThrRS) inhibitor with an IC50 of 1.4 µM and a Kd of 1.36 µM against Salmonella enterica ThrRS (SeThrRS). ThrRS-IN-1 simultaneously targets the tRNAThr and L-threonine binding pockets of ThrRS. ThrRS-IN-1 shows potent antibacterial activities[1].
Metrifonate is an irreversible organophosphate acetylcholinesterase inhibitor that is used as an insecticide for the control of flies and roaches.
Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 22 μM in an enzyme assay using rat liver microsomes[1].
Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside (compound 1) is a lignan with anti-HBC activity. Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside targets HBV surface antigen with IC50s of 0.58 mM (HBsAg) and >2.4 mM (HBeAg). Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside can be isolated from star anise[1].
Brevicompanine B, a diketopiperazine alkaloid, is an antiplasmodial agent. Brevicompanine B is active against the malaria parasite Plasmodium falciparum 3D7 IC50 of 35 mg/mL[1].
Columbianetin Acetate is a phytoalexin associated with celery (Apium graveolens) resistance to pathogens during storage. Columbianetin exhibits excellent anti-fungal and anti-inflammatory activity[1][2].
4-Hydroxybenzoic acid-13C is the 13C labeled 4-Hydroxybenzoic acid[1]. 4-Hydroxybenzoic acid, a phenolic derivative of benzoic acid, could inhibit most gram-positive and some gram-negative bacteria, with an IC50 of 160 μg/mL[2].
Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
SU0268 is a potent and specific inhibitor of 8-Oxoguanine DNA glycosylase 1 (OGG1). SU0268 regulates inflammatory responses during Pseudomonas aeruginosa infection[1][2][3].
RSV L-protein-IN-5 (compound E) is a potent inhibitor of Respiratory syncytial virus (RSV) (EC50=0.1 μM). RSV L-protein-IN-5 inhibits Polymerase (IC50=0.66 μM)，and blocks RSV mRNA synthesis by inhibiting guanylation of viral transcripts. RSV L-protein-IN-5 shows moderate cytotoxicity (CC50=10.7 μM，HEp-2)，also exhibits activity and lowers virus titers in mouse models of RSV infection[1].
Yadanzioside L is a quassinoid and shows anti-tobacco mosaic virus (TMV) activity (IC50=4.86 μM)[1].
2-Hydroxycinnamic acid is isolated from the methanol extract of Cinnamomum cassia. 2-Hydroxycinnamic acid shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC50 of 0.3 mM[2]
Buforin II, derived from buforin I, a protein isolated from the stomach of the Asian toad Bufo bufo gargarizans, is a potent antimicrobial peptide. Buforin II has antimicrobial activity against a broad spectrum of Gram-positive and Gram-negative bacteria[1].
(±)-Nirtetralin is an isomer of Nirtetralin, which inhibits growth of hepatitis E virus (HEV) in HepaRG cells[1].
Valganciclovir (hydrochloride), the L-valyl ester of ganciclovir, is actually a prodrug for ganciclovir. Valganciclovir is an antiviral medication used to treat cytomegalovirus infections.IC50 Value: Target: CMVin vitro: In cell culture model systems using Caco-2 cells for PEPT1 and SKPT cells for PEPT2, valganciclovir inhibited glycylsarcosine transport mediated by PEPT1 and PEPT2 with K(i) values (inhibition constant) of 1.68+/-0.30 and 0.043+/- 0.005 mM, respectively. The inhibition by valganciclovir was competitive in both cases [1].in vivo: 37 patients were enrolled; 19 patients received treatment with VGV and 18 patients received treatment with GCV. The VGV was not inferior in efficacy to GCV as pre-emptive therapy, with rates of viral clearance at 28 days of 89.5% and 83%, respectively (P-value for non-inferiority = 0.030). Toxicities were similar between the 2 arms. No patients developed CMV disease [2]. Patients being treated with an alemtuzumab-containing regimen received prophylaxis with either valaciclovir 500 mg orally daily orvalganciclovir 450 mg orally twice daily. None of the 20 patients randomized to valganciclovir experienced CMV reactivation (P = .004) [3].
A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively; inhibits cancer cell growth, modulates P-glycoprotein, and synergizes with doxorubicin in MCF7 and MCF ADR cells with IC50 in nanomolar range; increase G0-G1-phase fraction and caspase-independent apoptosis, also reduces P-gp expression.
Closantel-13C6 is the 13C6 labeled Closantel. Closantel is a halogenated salicylanilide with a potent anti-parasitic activity. Closantel is a potent and highly specific Onchocerca volvulus chitinase (OvCHT1) inhibitor with an IC50 of 1.6 μM and a Ki of 468 nM. Closantel inhibits the O. volvulus L3 to L4 molt of developing.
GS-704277 is an alanine metabolite of Remdesivir. Remdesivir, a nucleoside analogue with effective antiviral activity, is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
BRD-8000.3, as a specific EfpA inhibitor, is a narrow-spectrum, bactericidal antimycobacterial agent with good wild-type activity. BRD-8000.3 can be used for the research of tuberculosis[1].
Zinlirvimab is a humanized IgG1-λ2, HIV neutralising antibody targeting to HIV-1 gp120 envelope glycoprotein (IIIB gp120 V3 loop)[1][2].