Monensin B is a polyketide produced by Streptomyces cinnamonensis. Fermentations of Streptomyces cinnamonensis produce a mixture of Monensin A and Monensin B in a ratio dependent upon the relative concentrations of ethylmalonyl-CoA and methylmalonyl-CoA[1].
Junipediol A is a natural product, that can be isolated from the aerial parts of Juniperus phcenicea[1].
Nantenine is a serotonergic receptor antagonist. Nantenine selectively inhibits the contractile response of tissues to serotonin. Nantenine can be isolated from Nandina domestica[1].
Fraxamoside is a competitive xanthine oxidase inhibitor with an IC50 of 16.1 μM and a Ki of 0.9 μM[1].
Ms-PEG6-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
2,4-Pyrimidinediamine with linker is a patent compound in WO2013055780A1, Page 71; multikinase inhibitor and has a -NH2 terminal linker for further synthesis.Simultaneous detection of multiple protein kinases in tissue samples in the diagnosis and treatment of diseaseBy Johnson, Gary; Duncan, James S.; Whittle, Martin C.; Jian, Jin From PCT Int. Appl. (2013), WO 2013055780 A1 20130418.
Sitagliptin-d4 (MK-0431-d4) phosphate is the deuterium labeled Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1][2].
5,7-Dihydroxy-4-methylcoumarin is a coumarin derivative from Mexican tarragon[1].
S-Benzylglutathione is a competitive glutathionase inhibitor. S-Benzylglutathione is converted to the corresponding cysteine derivatives by rat kidney microsomes. S-Benzylglutathione can be used for the research of metabolic breakdown of glutathione by the glutathionase system[1].
3-[[2-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]-2-oxoethyl]amino]benzamide is a 2-(3,4-dimethoxyphenyl)ethylamine derivative for oral administration at an exploratory stage of new drug development.
Masticadienolic acid is an antitumor agent via increasing the production of nitric oxide (NO). Masticadienolic acid also increases the release of NO in resting macrophages[1].
S-acetyl-PEG3-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
p-SCN-Bn-DOTA is a bifunctional chelating agent. p-SCN-Bn-DOTA can simultaneously chelate radionuclides and link monoclonal antibody for radioimmunotherapy of tumor[1][2].
Antiviral agent 34 is a potent and orally active antiviral agent against influenza A and B subtypes with an EC50 value of 0.8 nM for H1N1 proliferation. Antiviral agent 34 derivatives inhibited influenza virus proliferation by targeting influenza virus RNA-dependent RNA polymerase. Antiviral agent 34 can be used for influenza virus research[1].
5'-O-DMT-N6-Me-2'-dA is a nucleoside with protective and modification effects.
PROTAC Linker 18 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 18 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Protease K is a nonspecific serine protease that is useful for general digestion of proteins. Protease K is active in the presence of SDS or urea and over a wide range of pH (4-12), salt concentrations, and temperatures[1].
Gymnoside IX (compound 2) can be isolated from the methanolic extract from the tubers of Gymnadenia conopsea[1].
SRPK-IN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC50s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect[1].
Lanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.
SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM[1].
N-Desethyl amodiaquine is the major biologically active metabolite of Amodiaquine. N-Desethyl amodiaquine is an antiparasitic agent. IC50 values for strains V1/S and 3D7 are 97 nM and 25 nM, respectively[1].
Prepro VIP (111-122), human is a prepro-vasoactive intestinal polypeptide (VIP)–derived peptide, corresponding to residues 111-122. VIP is present in the peripheral and the central nervous systems where it functions as a nonadrenergic, noncholinergic neurotransmitter or neuromodulator[1][2].
NF110 is a P2X3 receptor antagonist (Ki = 36 nM) and inactive toward P2Y receptors stably expressed (IC50s > 10 M). NF110 blocks alphabeta-methylene-ATP-induced currents (IC50 = 527 nM) in rat dorsal root ganglia neurons[1].
AJ2-30 is a SLCl5A4 inhibitor. AJ2-30 inhibits TLR9-mediated B cell activation. AJ2-30 block endogenous NOD signaling in human and mouse macrophages. AJ2-30 can be used for research of inflammation[1].
EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity[1].
GS-9256 is a selective HCV NS3 protease inhibitor. GS-9256 has good pharmacokinetic properties and antiviral activity[1].
6-trans-leukotriene B4 is a neutrophil chemotaxin in the guinea pig dermis[1].
Macrocarpal C can be isolated from the 95 % ethanol extract of fresh leaves of E. globulus. Macrocarpal C inhibits the growth of T. mentagrophytes via an increase in the permeability of the fungal membrane. Macrocarpal C increases the production of intracellular ROS and? induces apoptosis as a consequence of DNA fragmentation[1].
Moguisteine(BBR-2173) is a novel peripheral non-narcotic antitussive drug.Target: OthersMoguisteine is a novel peripheral nonnarcotic antitussive agent that has proved to be as active as codeine in several experimental models of induced cough in guinea-pigs and dogs. It acts neither through the opiate receptors nor on the cough centre, and its action is possibly mediated by the interaction with rapidly adapting irritant receptors along the tracheobronchial tree. In controlled clinical trials, moguisteine has been shown to be safe and to effectively reduce cough associated with such respiratory disorders as acute upper respiratory tract infection, chronic bronchitis, pulmonary fibrosis and malignancies [1, 2].