N-(Methoxycarbonyl)-D-valine methyl ester is an amino acid derivative that can be used for compound synthesis[1].
SARS-CoV-2 3CLpro-IN-16 (Compound 3a) is a covalent SARS-CoV-2 3CLpro inhibitor (IC50s: 2.124 μM). SARS-CoV-2 3CLpro-IN-16 binds to the active site and forms a covalent bond with Cys145 of 3CLpro[1].
Cyclosporin is a cyclic decapeptide that could be isolated form the soil fungi Tolypocladium inflatum. Cyclosporin is an immunosuppressant thought to bind to cyclophilin in T-lymphocytes[1].
WAY-608119 is an active molecule.
ML354 is a selective PAR4 antagonist with an IC50 of 140 nM[1].
Cobitolimod is a DNA oligonucleotide agonist of TLR-9 with anti-inflammatory activity. Cobitolimod suppresses Th17 cells and induces anti-inflammatory FoxP3 and IL-10 expression, inhibiting the IL-17 signaling pathway[1].
SCR-1481B1 (c-Met inhibitor 2) is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.
Influenza Matrix Protein (61-72) is a peptide fragment derived from matrix protein of influenza viruses, corresponds to amino acids 61-72. Influenza Matrix Protein (61-72) is a specific epitope which can induce CD4+ T-cell response[1].
Saphenamycin is an antibiotic from a strain of Streptomyces.
Fosetyl-aluminum (Fosetyl-Al) is an active ingredient in many fungicides against downy mildew. Fosetyl-aluminum is used to control many diseases caused by Phytophthora spp. on agricultural and horticultural crops[1][2].
cis-Tiliroside, a kaempferol derivative, is a flavonoid glycoside. cis-Tiliroside exhibits better cytotoxic activity than trans-Tiliroside in A549 cell line[1].
Tr-PEG3-OH is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
2R,4S-Sacubitril is the impurity of Sacubitril. Sacubitril is approved by the Food and Drug Administration for use in combination with valsartan for the treatment of patients with heart failure.
IDO1-IN-2 (compound 16) is a potent and selective IDO1 inhibitor with IC50s of 81 nM, 59 nM (mouse) and 28 nM (rat), respectively. IDO1-IN-2 has anti-cancer activity[1].
L-β-Homolysine dihydrochloride is a lysine derivative[1].
Isoarjunolic acid (2α,3α,23-Trihydroxyolean-12-en-28-oic acid) is a triterpenoid, can be isolated from the stems of Cornus kousa. Isoarjunolic acid could have free radical scavenging activity and elastase inhibition activity [1].
UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH1/2 with IC50s of 10 nM and 45 nM, repectively.
(Des-His6)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH; HY-106373). ACTH is a polypeptide tropic hormone produced by the anterior pituitary gland, regulating cortisol and androgen production[1].
Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.Target: AntibacterialGatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Gatifloxacin had activity equal to that of tosufloxacin and activity more potent than those of norfloxacin, ofloxacin, ciprofloxacin, and sparfloxacin against the second-step mutants (grlA gyrA; gatifloxacin MIC range, 1.56 to 3.13 microg/ml) and had the most potent activity against the third-step mutants (grlA gyrA grlA; gatifloxacin MIC range, 1.56 to 6.25 microg/ml), suggesting that gatifloxacin possesses the most potent inhibitory activity against singly mutated topo IV and singly mutated DNA gyrase among the quinolones tested [1].Ophthalmic gatifloxacin 0.3% is at least as effective as ciprofloxacin at healing corneal ulcers infected with Pseudomonas aeruginosa when gatifloxacin is administered less frequently than ciprofloxacin. Trends favored gatifloxacin in fluorescein retention scores [2].Clinical indications: Bacterial infection FDA Approved Date: Toxicity: Hepatotoxicity; Acute pancreatitis [3]; Torsades de pointes [4]
Tyk2-IN-9 (Compound 26) is a selective Tyk-2 inhibitor with IC50s of 0.076 and 1.8 nM for TYK2-JH2 and JAK1-JH2, respectively. Tyk2-IN-9 can be used for the research of inflammatory or autoimmune disease[1].
N-(2,4-Dinitrophenyl)glycine is a Glycine (HY-Y0966) derivative[1].
Ximelagatran (H 376/95) is an orally active thrombin inhibitor that selectively and competitively inhibits both free and clot-bound thrombin. Ximelagatran is an anticoagulant agent with a rapid onset of anticoagulant effect, predictable, dose-dependent pharmcokinetics and pharmacodynamics[1][2].
Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity[1]. Phortress free base leads to DNA damage and cell cycle arrest[2].
Cyclopropane-carbonyl Chloride-d5 is the deuterium labeled Cyclopropanecarboxylic acid chloride[1].
Microcystin-LF is a bacterial metabolite. Microcystin-LF is a phenylalanine variant of Microcystin-LR. Microcystin-LF has cellular toxicity on Caco-2 cells[1][2].
6-Methylpurine riboside is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM[1].
Triacetonamine is useful as an intermediate for the synthesis of pharmaceutical products, pesticides and photostabilizers for polymers. Triacetonamine is an artifact of plant and fungal extracts using acetone and ammonium hydroxide or natural occurrence of ammonium salts in various steps of the isolation procedures. TAA is the main component of the pyrolysis oil[1].
EP3 is an antimicrobial peptide. EP3 has antibacterial and antifungal activities. EP3 inhibits E. gallinarum, P. pyocyanea, A. baumanii, K. terrigena with a MIC value of 12.85 μg/mL. EP3 also shows antitumor activity against cancer cells, and induces cell apoptosis[1].