Azido-PEG2-hydrazide-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
8-O-Acetylharpagide is an iridoid isolated from Ajuga reptans with antitumoral, antiviral, antibacterial, and anti-inflammatory activities. 8-O-Acetylharpagide also has a biological activity on isolated smooth muscle preparations from guinea pig[1][2].
Peimine(Dihydroisoimperialine; Verticine) is a natural compound with good anti-inflammatory effects in vivo.IC50 value:Target:Peimine (0-25 mg/L) significantly inhibited tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-1β, and increased IL-10 production. Furthermore, peimine significantly inhibited the phosphorylation of p38, ERK and c-jun N-terminal kinase (JNK) as well as decreased p65 and IκB.
Mellein is an antibiotic isolated from culture fluids of this Aspergillus[1].
DSPE-mPEG is a PEG-based phospholipid. DSPE-mPEG-2000 can be used to synthesis liposomes for delivering cancer agents[1][2].
BMS-191011 (BMS-A) is an opener of the large-conductance, Ca2++-activated potassium (maxi-K) channel, effective in stroke models[1].
AU1235 is an adamantyl urea inhibitor of Mycobacterium tuberculosis.
Reproxalap (ADX-102) is a reactive aldehyde species (RASP) sequestering agent for the treatment of dry eye. Reproxalap (ADX-102) covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal[1][2].
Lometraline hydrochloride is an aminotetralin derivative and can be used for Parkinson's disease research[1].
(R)-Taltobulin ((R)-HTI-286) can be used as a reference substance[1].
LY306669 is a potent and selective leukotriene B4 (LTB4) receptor antagonist that can be used for the research of lung injury[1].
PD-1/PD-L1-IN-19 (Example 22) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-19 blocks PD-1/PD-L1 with the IC50 of 62.3 nM. PD-1/PD-L1-IN-19 can be used for the research of cancers, infectious diseases and autoimmune diseases[1].
Pramlintide is a polypeptide analogue of human amylin. Pramlintide is an antidiabetic, is antineoplastic in colorectal cancer[1].
C25-140, a first-in-class TRAF6-Ubc13 inhibitor, directly binds to TRAF6, thereby blocks the interaction of TRAF6 with Ubc13 and as a consequence lowers TRAF6 activity. C25-140 expands studying the impact of the ubiquitin system on immune signaling and underscores the importance of TRAF6 E3 ligase activity in psoriasis and rheumatoid arthritis (RA)[1].
cis-β-Terpineol, a monoterpene compound, can be isolated from the aerial parts of A. turcomanica. However, the stems, leaves and flowers of P. turkmen showed antibacterial activity[1].
Sirtuin modulator 5 is a sirtuin modulating agent. Sirtuin modulator 5 can activate SIRT1 with a DC50 value of <50 μM. Sirtuin modulator 5 can be used for increasing the lifespan of a cell and used for the research of variety of diseases including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity[1].
Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD). IC50 value:Target: M3 receptorPreclinically, aclidinium showed potent antagonism of human muscarinic receptors, with a long residence time at M3 receptors and a shorter residence time at M2 receptors, indicating the potential to provide sustained bronchodilation. Aclidinium is rapidly hydrolysed in human plasma, unlike other currently available antimuscarinics including tiotropium. Early clinical studies in healthy subjects have confirmed the low systemic bioavailability and favourable safety profile of single and multiple doses of aclidinium. In a subsequent Phase IIb study, which included 464 patients with moderate to severe COPD, aclidinium displayed long-lasting bronchodilatory activity and was well tolerated.
PythiDC is a selective collagen prolyl 4-hydroxylase (CP4H1) inhibitor with an IC50 value of 4.0 μM. PythiDC can be used as a CP4H probe and also can be used for the development of a new class of antifibrotic and antimetastatic agents[1].
Acanthoside B is a potential bioactive lignan with anti-inflammatory and anti-amnesic activities. Acanthoside B can be used for alzheimer's disease and lung inflammation research[1]
Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution[1][2].
AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts[1].
[Ala17]-MCH, a MCH analogue (HY-P1525A), is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2[1].
Picamilon is a derivative of γ-aminobutyric acid that has nootropic effect[1].
BuChE-IN-3 (Compound C4) is a potent inhibitor of BuChE with an IC50 of 8.3 nM. BuChE-IN-3 exhibits mild antioxidant capacity, nontoxicity, lipophilicity and neuroprotective activity[1].
Rocatinlimab (AMG 451) (KHK4083) is a fully human, non-fucosylated, immunoglobulin G1 (IgG1) anti-OX40 monoclonal antibody. Rocatinlimab can be used for the research of atopic dermatitis (AD)[1].
Pamiparib is a PARP inhibitor which can be used for the treatment of various cancers including the solid tumor, extracted from patent WO 2013097225 A1.
Methylergometrine (Methylergonovine) is an orally active 5-HT2B ligand agonist. Methylergometrine can be used as oxytocin and has protective effect on postpartum hemorrhage[1][2][3].
Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
5-(3-Azidopropyl)uridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.IC50 value:Target: Ral GTPase inhibitorRBC8 or BQU57 treatment showed no further inhibition of colony formation after Ral knockdown. RBC8 and BQU57 showed favorable properties that define good drug candidates. To test the effect of Ral inhibitors on xenograft tumor growth, nude mice were inoculated subcutaneously with H2122 human lung cancer cells and treated intraperitoneally with 50 mg/kg/d of RBC8 for 21 days (except weekends). RBC8 inhibited tumor growth to a similar extent as dual knockdown of RalA and RalB.