QST4 has antitubercular activity, with the MIC value of 6.25 μM in Mycobacterium tuberculosis H37Rv[1].
Indeloxazine hydrochloride is a 5-HT receptor and norepinephrine (NE) reuptake inhibitor. Indeloxazine hydrochloride is an antidepressant and cerebral activator[1].
Quininic acid, purified from Eucalyptus globulus, cinchona bark, and other plant products, is the most abundant organic acid[1].
Hydroxytyrosol (DOPET) is a phenolic compound drawn from the olive tree and its leaves with anti-oxidant, anti-atherogenic, anti-thrombotic, antimicrobial, anti-inflammatory and anti-tumour effects[1][2].
Spiramide (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT2 versus 5-HT1C (Ki=4300 nM) receptors. Spiramide exhibits antipsychotic activity[1][2][3].
ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively.
3’-Deoxy-3’,5-difluorocytidine 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].
E3 ligase Ligand 5 is a ligand of E3 ligase, extracted from patent US 20160058872A1, Paragraph 0515. E3 ligase Ligand 5 can be used in PROTAC technology.
Coumarin 6H, a Coumarin (Coumarin (HY-N0709)) derivative, is a laser dye. The fluorescence emission of Coumarin 6H can be enhanced by hydrogen bonding interactions[1][2].
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer[1].
Boc-Cystamine-Poc (compound H4) is a click chemistry reagent with cystamine building block[1].
4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic acid disodium is a fluorescent dye. 4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic acid disodium can be used to demonstrate retrograde axonal transport to label secondary antibodies and as a fluorescent whole cell stain[1].
PBP10 is a cell permeable and selective gelsolin-derived peptide inhibitor of formyl peptide receptor 2 (FPR2) over FPR1[1]. PBP10 is a 10-AA peptide with rhodamine conjugated at its N terminus, exerts bactericidal activity against gram-positive and gram-negative bacteria and limits microbial-induced inflammatory effects[2].
Ramifenazone-d7 (Isopropylaminoantipyrine-d7) is the deuterium labeled Ramifenazone. Ramifenazone (Isopropylaminoantipyrine) is a pyrazole derivative and acts as a non-steroidal anti-inflammatory agent (NSAID). Ramifenazone has analgesic, antipyretic, anti-inflammatory and antimicrobial activities[1][2].
Azido-PEG7-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Contezolid acefosamil sodium (MRX-4), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid acefosamil sodium (MRX-4) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI)[1][2].
R)-DPN (compound 3) is a selective ERβ ligand with EC50s of 2.9, 0.8 nM for ERα and ERβ, respectively. (R)-DPN shows a very high affinity and potency preference for ERβ over ERα. (R)-DPN shows cytoxicity for HEC-1 and U2OS cells with EC50s of 286, 205 nM, respectively[1].
2,3,4,5-Tetracaffeoyl-D-Glucaric acid is a caffeoyl-D-glucaric acid derivative isolated from the Genus Gnaphalium[1].
Isoquinoline-d7 is the deuterium labeled Isoquinoline[1]. Isoquinoline is an analog of?pyridine. Isoquinoline structural-based alkaloids, such as tropoloisoquinoline, phthalideisoquinoline, and naphthylisoquinoline has anti-cancer activities[2].
Pyronin B is an organic cationic dye used for the staining of bacteria, mycobacteria and ribonucleic acids. Pyronin B is also used as a small hydrophobic (SH) protein channel inhibitor[1][2].
Danburstotug (IMC-001) is an IgG1-lambda anti-CD274 (PDL1, B7 homologue 1, B7H1) humanized monoclonal antibody. Danburstotug also is immunostimulant and antineoplastic[1].
(S)-4-Methyl-2-(methylamino)pentanoic acid hydrochloride is a leucine derivative[1].
PGLa is an antimicrobial peptide. PGLa is known to be bacteriostatic against both Gram-positive and Gram-negative bacteria.
Vasicinol is a reversible inhibitor of sucrase (IC50: 250 μM). Vasicinol is a HbF inducer. Vasicinol also inhibits Angiotensin-converting Enzyme (ACE). Vasicinol is apyrroquinazoline alkaloid that can be isolated from Adhatoda vasica[1][2].
Fosnetupitant (Pronetupitant) a methylene phosphate prodrug of Netupitant. Fosnetupitant (Pronetupitant) exhibits a pKi of 9.5 for human NK1 receptor[1].
Glyoxalase I inhibitor 6 (Compound 9j) is a glyoxalase I (Glo-I) inhibitor with an IC50 of 1.13 μM. Glyoxalase I inhibitor 6 can be used as anticancer agent with low toxicity[1].
MAP4K4-IN-17 is a potent and highly selective MAP4K4 inhibitor with IC50 of 14.9 nM, showes improved overall drug-like properties compared to PF-06260933; a lead compound for advanced preclinical development.
PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.
β-catenin peptide is a 8-aa peptide, and can promote thymocyte positive selection.
Azido-PEG5-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].