Halofuginone (RU-19110) is a less-toxic form of Febrifugine, which is isolated from the plant Dichroa febrifuga[1]. Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM[2]. Halofuginone attenuates osteoarthritis (OA) by inhibition of TGF-β activity[3].
1-Heptadecanol is a long-chain primary alcohol with antibacterial activity from Solena amplexicaulis leaves[1].
Antiasthmatic Compound 1 is an antiasthmatic agent, which can be used to treat allergic asthma.
Celecoxib is a selective COX-2 inhibitor with an IC50 of 40 nM.
Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 can be used to treat inflammatory pain[1].
PAR-4 Agonist Peptide, amide is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist.
Dehydrobruceine A is a low potent antitrypanosomal agent, with an IC50 of 88.5 nM for Plasmodium falciparum[1].
Pumecitinib is a Janus kinase (JAK) inhibitor with anti-inflammatory activity[1].
Letrazuril is a p-fluor analogue of diclazuril which can be used in the prevention and treatment of coccidia infections in domestic fowl.
BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
Diphenhydramine HCl (Benadryl), a histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations.Target: Histamine H1 receptorDiphenhydramine HCl (Benadryl), a histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects. Diphenhydramine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding.
9-(2-Carboxy-2-cyanovinyl)julolidine is a fluorescent molecular rotor. 9-(2-Carboxy-2-cyanovinyl)julolidine can be used to bind to IgG and Fab, and preparing antibodies[1].
AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist[1].
LAS191859 is an orally active, potent and selective CRTh2 antagonist with an IC50 of 9.58 nM against human CRTh2. LAS191859 can be used for the research of chronic asthma[1].
Mycophenolic acid is an an immunosuppresant drug and has potent anti-proliferative activity.Target: OthersMycophenolic acid(MPA) is an immunosuppressant drug used to prevent rejection in organ transplantation. It inhibits an enzyme needed for the growth of T cells and B cells. MPA did not block the initial phase of viral translation but did interfere with viral protein synthesis in the amplification phase. Quantitative RT-PCR demonstrated that MPA prevented the accumulation of viral positive- and negative-strand RNA as the infection proceeded. MPA inhibits flavivirus infection by preventing synthesis and accumulation of viral RNA [1]. The effects of mycophenolic acid (MPA) on DEN replication in monkey kidney (LLC-MK2) cells were examined. MPA (IC(50)=0.4+/-0.3 microM) inhibited DEN2 replication. Quantitative real-time RT-PCR of viral RNA and plaque assays of virions from DEN2-infected and MPA (10 microM) -treated cells showed a fivefold increase in defective viral RNA production by cells treated with each drug. suggesting that one mode of antiviral action of MPA is by inhibition of inosine monophosphate dehydrogenase and thereby depletion of the intracellular GTP pool [2].
Mosunetuzumab (BTCT-4465A) is a humanized, immunoglobulin G1-based bispecific antibody targeting CD20 (B cells) and CD3 (T cells). Mosunetuzumab redirects T cells to engage and eliminate malignant B cells and can be used for the research of relapsed or refractory (R/R) B-cell non-Hodgkin lymphomas (B-NHLs)[1].
Otilimab (GSK 3196165) is an anti-granulocyte-macrophage colony-stimulating factor (GM-CSF) humanized monoclonal antibody. Otilimab neutralises the biological function of GM-CSF by blocking the interaction of GM-CSF with its cell surface receptor[1].
HE3286, a synthetic derivative of the adrenal steroid β-AET, is an orally-active partially NF-κB inhibitor [1][2].
Dehydroandrographolide succinate (potassium sodium salt), extracted from herbal medicine Andrographis paniculata (Burm f) Nees, is widely used for the treatment of viral pneumonia and viral upper respiratory tract infections because of its immunostimulatory, anti-infective and anti-inflammatory effect[1][2].
CD73-IN-11 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-11 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022068929A1, compound 24)[1].
RIP1 kinase inhibitor 8 (Compound 77) is a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor with an IC50 of 20 nM. RIP1 kinase inhibitor 8 prevents necrotic cell death. RIP1 kinase inhibitor 8 shows a favorable pharmacokinetic profile in multiple species[1].
Vapaliximab (2D10) is a monoclonal antibody against human VAP-1[1].
Nucleoprotein (396-404) is the 396 to 404 fragment of lymphocytic choriomeningitis virus (LCMV). Nucleoprotein (396-404) is the H-2D(b)-restricted immunodominant epitope and can be used as a molecular model of viral antigen.
(-)-Stylopine ((S)-Tetrahydrocoptisine) is an enantiomer of Stylopine (HY-N0924). Stylopine is a major alkaloid component of the leaf of Chelidonium majus[1].
Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects[1][2].
SK1-IN-1 is a potent sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 58 nM.
BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCFFbxo3 catalyzed Fbxl2 ubiquitination. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1–TRAF6. BC-1215, interacts with ApaG to profoundly inhibit secretion of a broad spectrum of TH1 panel cytokines from human PBMC[1].
{Boc}-Phe-Leu-Phe-Leu-Phe ({Boc}-FLFLF) is a formyl peptide receptor (FPR) family antagonist that preferentially inhibit activity triggered through the formyl peptide receptor[1].
Anti-inflammatory agent 11 (compound 16) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 11 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 1.3 and 6.9 μM, respectively. Anti-inflammatory agent 11 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 11 can be used for tuberculosis (TB) research[1].