NSC260594 (NSC 260594) is a specific inhibitor of HIV-1 RNA packaging, which involves preventing the interaction of Gag with SL3 by stabilizing this small RNA stem-loop which then leads to stabilization of the global packaging signal region (psi or ψ); specifically blocks HIV-1 RNA encapsidation, binds to HIV-1 gRNA and exhibits potent antiviral activity; NSC260594 also is a small molecule inhibitor of the Escherichia coli condensin MukBEF, affects MukB directly.
C-215 is a novel inhibitor of mycobacterial membrane protein large 3 (MmpL3) with MIC90 of 16 uM against M. tuberculosis.
Antibacterial agent 123 (compound 111) is a potent membrane-disrupting agent to combat antibiotic-resistant Gram-positive bacteria[1].
Isobellidifolin, a xanthone, is a free radical scavenger and antioxidant compound. Isobellidifolin has potent antifungal effect[1].
Pentamidine(MP-601205) is an antimicrobial agent.Target: AntiparasiticPentamidine has a potent in vitro antiprotozoal activity. Pentamidine displays cytotoxic activity against L. infantum promastigotes with IC50 of 2.5 μM. 2.5 μM Pentamidine induces early programmed cell death in 49.6% of L. infantum promastigotes. 2.5 μM Pentamidine induces a notorious decrease in promastigotes in both G1 and S phases relative to the control-untreated samples (G1:77.0 vs 15.0%; S:11.0 vs 2.4% for control- and pentamidine-treated promastigotes, resp). Pentamidine is able to bind with calf-thymus DNA (CT-DNA) and induces conformational changes in the DNA double helix. Pentamidine also binds with ubiquitin to modifiy the β-cluster of ubiquitin [1]. Pentamidine is an inhibitor of phosphatase of regenerating liver (PRLs). 1 μg/mL of Pentamidine complete inhibits the activity of recombinant PTP1B in dephosphorylating a phos-photyrosine peptide. 10 μg/mL of Pentamidine completely inhibits the activities of recombinant PRL-1, PRL-2 and PRL-3 in dephosphorylating a phosphotyrosine peptide substrate. Incubation with Pentamidine (1 μg/mL) for 48 h reduces the activity of intracellular PRL phosphatases in transfected NIH3T3 cells by more than 85%. 10 μg/mL Pentamidine completely inhibits the growth of melanoma cell line (WM9), prostate carcinoma cell line (DU145 and C4-2), ovarian carcinoma cell line (Hey), colon carcinoma cell line (WM480), and lung carcinoma cell line (A549) which all express endogenous PRLs [2].
Biapenem is a parenteral carbapenem antibacterial agent with a broad spectrum.Target: AntibacterialBiapenem is a carbapenem antibiotic of in vitro antibacterial activity encompassing many Gramnegative and Gram-positive aerobic and anaerobic bacteria, including species producing β-lactamases. Biapenem is more stable than imipenem, mero-penem and panipenem to hydrolysis by human renal dihydropeptidase-I (DHP-I), and therefore does not require the coadministration of a DHP-I inhibitor. In randomised, nonblind or double-blind clinical trials, biapenem showed good clinical and bacteriological efficacy (similar to that of imipenem/ cilastatin) in the treatment of adult patients with intra-abdominal infections, lower respiratory infections or complicated urinary tract infections.
4',7-Dimethoxyisoflavone is isolated from the leaves of Albizzia lebbeck, which shows antifungal activity.
Pritelivir mesylate hydrate (BAY 57-1293 mesylate hydrate), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir mesylate hydrate is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2[1].
Valacyclovir hydrochloride hydrate is a potent antiviral agent. Valacyclovir hydrochloride hydrate can be used in the management of herpes simplex, herpes zoster and herpes B. Valacyclovir hydrochloride hydrate can be formulate ocular inserts for the treatment of ocular herpes. Valacyclovir hydrochloride hydrate is a prodrug and can be rapidly converted into acyclovir in vivo[1][2].
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease[2].
Tiadinil is a plant activator of systemic acquired resistance, boosts the production of herbivore-induced plant volatiles; insecticide agent.
Difloxacin hydrochloride is a broad-spectrum antibacterial drug. Difloxacin hydrochloride inhibits bacterial DNA gyrase and exhibits a concentration-dependant bactericidal effect by interference with the activity of DNA gyrase and topoisomerase IV[1].
Succinylsulfathiazole is a sulfonamide, it is an ultra long acting drug.
(+)-SJ733 is a clinical candidate for malaria which can also inhibit Na+-ATPase PfATP4.
Cleroindicin F ((-)-Rengyolone), a cleroindicin, is an antimicrobial agent. Cleroindicin F shows relatively high anticandidal activity against Candida strains with a MIC value down to 12.5 µg/mL[1].
Delavirdine mesylate is a potent non-nucleoside HIV-1 reverse transcriptase inhibitor (NNRTI) of HIV-1.
Moniliformin sodium salt is a potent, water-soluble mycotoxin isolate from Fusarium moniliforme.
SARS-CoV-2 Mpro-IN-9 (compound c7) is a nonpeptidic, noncovalent SARS-CoV-2 Mpro inhibitor (IC50=0.085 μM), with improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. SARS-CoV-2 Mpro-IN-9 inhibits viral replication (EC50=1.10 μM) in SARS-CoV-2-infected Vero E6 cells, while exhibits low cytotoxic effects (CC50>50 μM)[1].
Undecanoic acid-d2 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Sodium Houttuyfonate is a natural compound extracted from Houttuynia cordata, with anti-inflammatory and anti-fibrotic effects. Sodium Houttuyfonate ameliorates LPS induced mastitis by inhibiting the NF κB pathway[1][2].
Azulene (Cyclopentacycloheptene) is as an isomer of naphthalene with high anti-HIV activity. Azulene, isolated from the distillation of chamomile oil, is a scaffold in medicinal chemistry[1][2][3].
KPC-2-IN-1, boronic acid derivative, is a potent KPC-2 inhibitor with Ki of 0.032 μM. KPC-2-IN-1 enhances the activity of cefotaxime in KPC-2 expressing E. coli. KPC-2-IN-1 exhibits well tolerated in human HEK-293 cells, which can be used for the study of E. coli resistance to β-lactam antibiotics[1][2].
Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is a autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
Ibuzatrelvir (PF-07817883) is an antiviral agent, targeting to SARS-CoV-2 3CL protease. Ibuzatrelvir can be used to inhibit COVID-19[1].
Hepatitis b virus pre-s region (120-145) is a preS2 peptide that inhibits the binding of single-chain Fv fragment (scFv) or IgG to r-HBsAg[1].
Eberconazole nitrate is a dichlorinated imidazole derivative with antifungal activity. Eberconazole nitrate is more active than Clotrimazole, Ketoconazole, and Miconazole. Eberconazole nitrate has the potential for the research of dermatophytoses with a topical administration[1].
Extracellular death factor (EDF) is the only single signaling molecule involved in Escherichia coli quorum sensing, and can initiate MAZEF-mediated cell death. Extracellular death factor significantly amplifies the endoribonucleolytic activities of both MazF and ChpBK[1].
DL-Syringaresinol ((±)-Syringaresinol), a lignin, inhibits UVA-induced upregulation of MMP-1 by suppressing MAPK/AP-1 signaling in human HaCaT keratinocytes and dermal fibroblasts (HDFs). DL-Syringaresinol has antiphotoaging properties against UVA-induced skin aging. DL-Syringaresinol exhibits weak antimycobacterial activity against Mycobacterium tuberculosis H37Rv[1][2].
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria[2]. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
Omaciclovir (H2G) is a potent and selective inhibitor of herpesvirus replication. Omaciclovir is a nucleoside analog with antiviral activity[1].