Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity[1][2].
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM[1]. Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM[1][2].
Proguanil-d4 is the deuterium labeled Proguanil[1]. Proguanil, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor[2][3].
Deoxythymidine-5'-triphosphate (dTTP), a deoxynucleotide, can be used in deoxyribonucleic acid synthesis[1].
Dicloxacillin NaOH is a narrow-spectrum β-Lactam antibiotic of the penicillin class, is used to treat infections caused by susceptible Gram-positive bacteria, active against beta-lactamase-producing organisms such as Staphylococcus aureus.
DHODH-IN-9 (Compound 10k) is an azine-bearing analogue and is a human dihydroorotate dehydrogenase inhibitor. DHODH-IN-9 has antiviral effect with a pMIC50 of 7.4[1].
HIF-2α-IN-7 is a hypoxia inducible factor 2α (HIF-2α) inhibitor. HIF-2α-IN-7 can inhibit HIF-2α with an EC50 value of 6nM. HIF-2α-IN-7 can be used for the research of various types of diseases including cancer, liver disease, inflammatory disease, pulmonary diseases and iron load disorders[1].
MM3122 is a selective type II transmembrane serine protease (TMPRSS2) inhibitor with an IC50 value of 0.34 nM. MM3122 effectively blocks TMPRSS2, thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells[1].
Pyridaben-d13 is the deuterium labeled Pyridaben[1]. Pyridaben is a mitochondrial electron transport inhibitor (METI) acaricide that promotes the formation of damaging oxygen and nitrogen radicals. Pyridaben selectively inhibits complex I (NADH dehydrogenase) with an IC50 value of 2.4 nM (assay sites: rat liver and bovine heart mitochondria). Pyridaben also significantly inhibits rat mitochondrial mtNOS function[2][3].
Penicillin G potassium is a fast-acting antibiotic; used to treat bacterial infections that affect the blood, heart, lungs, joints, and genital areas.
Cap-dependent endonuclease-IN-26 is a cap-dependent endonuclease (CEN) inhibitor with an IC50 of 286 nM. Cap-dependent endonuclease-IN-26 shows antiviral activity against many influenza A and B strains[1].
Florfenicol, a commonly used veterinary antibiotic, is currently indicated for the treatment of bovine respiratory disease, and also used in aquaculture for the control of enteric septicemia in catfish. Florfenicol can induce early embryonic death in eggs, with an LC50 of 1.07 μg/g.
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K+ efflux, Ca2+ influx, and changes in membrane potential, and is related to channel formation[1][2].
Celgosivir (MBI 3253; MDL 28574; MX3253) is a novel α-glucosidase I inhibitor, an enzyme that plays a critical role in viral maturation by initiating the processing of the N-linked oligosaccharides of viral envelope glycoproteins.[1]
ARX-1796 (AV-006), an Avibactam prodrug, is an orally bioavailable β-lactamase inhibitor. Avibactam has a spectrum of inhibition of class A and C β-lactamases, including ESBLs, AmpC and Klebsiella pneumoniae carbapenemase (KPC) enzymes[1][2].
A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively; also potently inhibits FLT3, VEGFR2, Fyn, PDGFRα and VEGFR2; shows promising outcomes for the treatments of idiopathic pulmonary fibrosis (IPF).
8-Br-GTP, a GTP analog, is a competitive FtsZ polymerization and GTPase activity (Ki of 31.8 μM) inhibitor. 8-Br-GTP can be used for nucleic acid modification[1].
Isoleucyl tRNA synthetase-IN-2 (compound 36a) is a potent and selective isoleucyl-tRNA synthetase (IleRS) inhibitor, with a Ki,app of 114 nM[1].
Eubananin is an effective inhibitor of the ATPase activity of the SARS Coronavirus helicase with an IC50 value of 2.8 μM.
HIV-1 inhibitor-55 (compound 4d) inhibits WT HIV-1 with an EC50 value of 8.6 nM. HIV-1 inhibitor-55 also shows inhibitory potency against single and double HIV-1 mutants. HIV-1 inhibitor-55 can be used for the research of virus infection[1].
Kasugamycin hydrochloride (Ksg hydrochloride) is an antibiotic which binds both the 30S and 70S ribosome but not isolated 50S subunits. Kasugamycin hydrochloride (Ksg hydrochloride) mimics mRNA nucleotides to destabilize tRNA binding and inhibit canonical translation initiation[1][2].
Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity[1] [2][3].
Nicarbazin is an effective anticoccidial agent for chickens[1].
Morantel citrate is a veterinary anthelmintic agent that inhibits parasitic infections in cattle, sheep and goats. Morantel citrate paralyzes the nervous system of the parasite, helping the animal expel the dead parasite from the body[1].
CEF3 (SIIPSGPLK) corresponds to aa 13-21 of the influenza A virus M1 protein. The matrix (M1) protein of influenza A virus is a multifunctional protein that plays essential structural and functional roles in the virus life cycle.
CXCR4 antagonist 9 (Compound 2) is a CXCR4 antagonist with an IC50 of 15 nM. CXCR4 antagonist 9 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 1.3 nM[1].
KNI-102 is a potent anti-HIV agent with an IC50 value of 100 nM for HIV protease[1].
Cefditoren sodium (ME 1206) is a broad-spectrum, third-generation, oral cephalosporin antibacterial with enhanced stability against many common β lactamases. Cefditoren sodium has activity against Gram-negative organisms and Gram-positive organisms. Cefditoren sodium can be used in the research of infection diseases such as acute exacerbations of chronic bronchitis, community-acquired pneumonia (CAP), streptococcal pharyngitis/tonsillitis, or uncomplicated skin and skin structure infections[1][2].
Garvicin KS, GakA is a peptide at sizes of 34 amino acids to form bacteriocin garvicin KS (GarKS), with other 2 peptides, GakB, and GakC. Garvicin KS, GakA inhibits fibroblast viability and proliferation. Garvicin KS, GakA with GakB, is a potent combination with good peptide stability, antimicrobial efficacy, and fibroblast viability/proliferation effects. Garvicin KS peptides inhibit MSSA with MIC values in the order GakB >GakC >GakA[1].
17-GMB-APA-GA is an ADC Cytotoxin. 17-GMB-APA-GA is a potent HSP90 inhibitor and used for latent T. gondii infection research[1].