SARS-CoV-2-IN-39 (compound 21) is a SARS-CoV-2 inhibitor with an EC50 of 1 μM. SARS-CoV-2-IN-39 against SARS-CoV-2 by inhibiting of SKP2 protein and stabilizing BECN1[1].
DM8966 exhibits potent antibacterial activity against gram-positive and -negative bacteria.
HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC50s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC50 > 221 μM) and a favorable in vitro microsomal stability[1].
RRx-001 is a potent inhibitor of G6PD. RRx-001 shows potent antimalarial, although as a single agent, the drug sensitivity testing indicated that higher dose of RRx-001 was required to inhibited 50 % of the parasite's activity (IC50 = 0.14 ± 0.04 ug/ml).IC50 value: 0.14 ± 0.04 ug/ml [1]Target: G6PDin vitro: RRx-001 is a novel, systemically non-toxic, epigenetic anticancer agent for multiple tumour types, with activity mediated through increased nitric oxide (NO) production and PPP inhibition. [1]in vivo: RRx-001is a novel, nonexplosive molecule modified from a class of solid rocket propellants, has shown promise as a novel cancer therapeutic agent in a number of cell lines and tumor models. In mouse models, RRx-001 administered intravenously as a single agent was equipotent to cisplatin while better tolerated. RRx-001 also showed activity as a radiosensitizer in both in vitro and in vivo models. The activity of RRx-001 is thought to be associated with a nucleophilic substitution by circulating thiol compounds and covalent binding of RRx-001 to cysteinyl residues in Hb, followed by the generation of nitrogen oxides. [2]
Antifungal agent 73 (compound A32) is an antifungal agent for azole-resistant candidiasis. Antifungal agent 73 disrupts the fungal cell wall and cell membrane. Antifungal agent 73 shows potent in vivo antifungal activity against pathogenic fungi and fluconazole-resistant strains[1].
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].
Benzoic acid-d5 is a deuterium substitute for Benzoic acid. Benzoic acid is an aromatic alcohol that occurs naturally in many plants and is a common additive in food, beverages, cosmetics and other products. Benzoic acid can act as a preservative by inhibiting bacteria and fungi[1][2].
Colistin is a polypeptide antibiotic which inhibits gram-negative bacteria by binding to lipopolysaccharides and phospholipids in the outer cell membrane of gram-negative bacteria.
Hikizimycin is a potent anthelmintic and antibacterial natural product.
2,4′-Dichloroacetanilide is a fungistatic agent. 2,4′-Dichloroacetanilide inhibits T. asteroides with a MIC value of 6.25 μg/mL[1].
β-?Solamarine is an antibacterial agent[1].
Sulfametrole is an orally active and potent antibacterial. Sulfametrole can be used for infections research, such as HIV, severe pneumonia and UTIs (urinary tract infections)[1][2].
Anti-infective agent 1 (compound 3a) is a potent and selective antiprotozoal and antimycobacterial agent. Anti-infective agent 1 shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 10.95 and 0.06 μM, respectively. Anti-infective agent 1 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 8 μg/mL[1].
Closthioamide is a potent inhibitor of bacterial DNA gyrase and highly active against Ec, MRSA, VRE and Mv), with MICs of 9.00 μM, 0.58 μM, 0.58 μM and 72.03 μM respectively.
SARS-CoV-2-IN-7 inhibits viral replication with a nanomolar IC50 value (844 nM) in SARS-CoV-2-infected Vero E6 cells.
Tiadinil is a plant activator of systemic acquired resistance, boosts the production of herbivore-induced plant volatiles; insecticide agent.
Peretinoin is an oral acyclic retinoid, inhibits HCV RNA amplification and virus release by altering lipid metabolism.Target: HCVin vitro: Peretinoin is an acyclic retinoid, improves the hepatic gene signature of chronic hepatitis C following curative therapy of hepatocellular carcinoma. Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors, such as retinoid X receptor and retinoic acid receptor. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism. Peretinoin suppresses the RNA replication of H77S.3/GLuc2A most efficiently and its EC50 was 9 μM. Peretinoin may reduce the recurrence of hepatocellular carcinoma (HCC) following surgical ablation of primary tumours. Peretinoin inhibits RNA replication for all genotypes and showed the strongest antiviral effect among the retinoids tested. in vivo: In addition, Peretinoin prevents the development of hepatoma in several different hepatoma models.
2'-Hydroxy-3,4,4',6'-tetramethoxychalcone (Compound 5) has antibacterial activity, with a MIC value of 10 μg/mL for E. coli and S. epidermis. 2'-Hydroxy-3,4,4',6'-tetramethoxychalcone can be isolated from Piper obliquum[1].
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.
Apramycin(Nebramycin II) is an aminoglycoside antibiotic used in veterinary medicine. IC50 value:Target: Apramycin stands out among aminoglycosides for its mechanism of action which is based on blocking translocation and its ability to bind also to the eukaryotic decoding site despite differences in key residues required for apramycin recognition by the bacterial target. The drug binds in the deep groove of the RNA which forms a continuously stacked helix comprising non-canonical C.A and G.A base pairs and a bulged-out adenine. The binding mode of apramycin at the human decoding-site RNA is distinct from aminoglycoside recognition of the bacterial target, suggesting a molecular basis for the actions of apramycin in eukaryotes and bacteria.
Triclopyricarb (SYP-7017) is a strobilurin fungicide that can be used in crops disease control. Triclopyricarb inhibits mycelial growth with EC50 values ranged from 0.006 µg/mL to 0.047 µg/mL[1][2].
Chitinase has partial lysozyme activity and is widely found in bacteria, fungi, animals and some plants. Chitinase belongs to the glycosyl hydrolase family. Chitinase catalyzes chito-oligosaccharide hydrolysis[1].
(+)-SJ733 is a clinical candidate for malaria which can also inhibit Na+-ATPase PfATP4.
(±)-Alliin is the main active component of garlic. (±)-Alliin is a putative inhibitor of the main protease of SARS-CoV-2 (Mpro)[1].
Cloxacillin sodium exhibits antibiotic efficacy, with a MIC of 256 mg/L for Staphylococcus aureus 25923[1][2][3].
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.
Methylisothiazolinone is a synthetic biocide and preservative that can be widely used in both industrial and consumer products. Methylisothiazolinone as a preservative in cosmetic and toiletrie products[1].