Rocastine is a selective, nonsedating H1 antagonist, acting as an antihistamine.
Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity[1].
Phytohemagglutinin (PHA) is a lectin, obtained from the red kidney bean that binds to the membranes of T-cells, stimulates metabolic activity, cell division, and involves inflammatory pathways. Phytohemagglutinin (PHA) induces apoptosis via increasing proapoptotic protein Bax and activating caspases-3[1][2][3].
Propargyl-Tos is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Tenalisib R Enantiomer is an R enantiomer of Tenalisib.
Landipirdine is a selective antagonist of 5-HT6R. Landipirdine has great effect on the hERG pharmacophore[1].
TLR7/8 agonist 4 (compound 41) is a potent TLR7/8 agonist. TLR7/8 agonist 4 has anti-cancer activity[1].
Dimethyl 3,3'-disulfanediyl(2R,2'R)-bis(2-aminopropanoate) dihydrochloride is a cysteine derivative[1].
Biotinyl-Amylin (mouse, rat) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development[1].
PROTAC BRD9-binding moiety 5 is a selective BRD9 binder with an IC50 value of 4.20 μM, can be used for the synthesis of PROTACs. PROTAC BRD9-binding moiety 5 has antiproliferative activity against cancer cells[1].
Z-D-MeAla-OH is an alanine derivative[1].
5-Naphthyl-beta-methylaminocarbony-3’-O-acetyl-2’-O-methyl-5’-O-DMTr-uridine is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
7′-Methoxylariciresinol is a phenylpropanoids that can be isolated from Crataegus pinnatifid[1].
Cetuximab sarotalocan (Cetuximab-IRDye-700DX) is an IRdye700DX (near-infrared photosensitizing dye) conjugate of Cetuximab (anti-EGFR monoclonal antibody). Cetuximab sarotalocan can be used for head and neck cancers research[1][2].
RX 67668 is a potent cholinesterase inhibitor with an IC50 of 5 μM for both acetylcholinesterase (AChE) and butyrylcholinesterase. RX 67668 can reverse the neuromuscular blockade induced by D-tubocurarine. RX 67668 is a muscle relaxant used to relieve skeletal muscle fatigue[1][2].
Cholesterol Pelargonate, a Cholesterol derivative, can be used as a triggered release liposome tested[1].
Tea polyphenol is the floorboard of phenolic compounds in tea. Tea polyphenol exhibits biological activity including antioxidant and anti-cancer activities, inhibition of cell proliferation, induction of apoptosis, cell cycle arrest and modulation of carcinogen metabolism[1].
Bletilloside A is a natural glucoside that could be found in the tubers ofBletilla striata[1].
2-amino-4-sulfobutanoic acid is an alanine derivative[1].
Fmoc-aminooxy-PEG2-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research[1][2][3][4].
MK-8262 is an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 53 nM and a log D of 5.3. MK-8262, a bistrifluoromethyl analogue, has the potential for coronary heart disease (CHD) correlated high-density lipoprotein (HDL) and low-density lipoprotein (LDL) research[1].
F992 is an antidiuretic peptide and vasopressin (antidiuretic hormone) analogue[1].
Rotundic acid, a triterpenoid obtained from I. rotunda, induces DNA damage and cell apoptosis in hepatocellular carcinoma through AKT/mTOR and MAPK Pathways. Rotundic acid possesses anti-inflammatory and cardio-protective abilities[1].
Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activates p53 signaling, which results in the induction of the apoptosis[1].
SPA70 is a potent and selective hPXR antagonist (IC50=0.51 uM) that interacts with the ligand-binding domain (LBD) of hPXR, inhibits hPXR in human hepatocytes and mouse models and enhances the chemosensitivity of cancer cells; displays highly selectivity over 10 other nuclear receptors (FXR, LXR, RXR, PPAR, etc.); antagonizes hPXR target genes induced by various hPXR agonists, blocks hPXR-mediated drug metabolism in vivo.
Foravirumab (CR4098) is a monoclonal antibody against rabies virus glycoprotein antigenic site III[1].
Ranolazine(RS-43285) is an antianginal agent with antiarrhythmic properties that achieves its effects via a novel mechanism of action (inhibition of the late phase of the inward sodium current), without affecting heart rate or blood pressure (BP). IC50 value:Target: sodium-dependent calcium channelRanolazine is currently approved for use in chronic angina. The basis for this use is likely related to inhibition of late sodium channels with resultant beneficial downstream effects. Randomized clinical trials have demonstrated an improvement in exercise capacity and reduction in angina episodes with ranolazine.
Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure.Target: ACEFosinopril is a phosphinic acid-containing ester prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is rapidly hydrolyzed to fosinoprilat, its principle active metabolite. Fosinoprilat inhibits ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Fosinopril may be used to treat mild to moderate hypertension, as an adjunct in the treatment of congestive heart failure, and to slow the rate of progression of renal disease in hypertensive individuals with diabetes mellitus and microalbuminuria or overt nephropathy [1-3].
TPB15 is an orally active and potent Hh (Hedgehog) signaling inhibitor. TPB15 markedly induces cell cycle arrest and apoptosis in MDA-MB-468 cells. TPB15 blocks Smo (Smoothened) translocation into the cilia and reduced Smo protein and mRNA expression. TPB15 inhibits the expression of the downstream regulatory factor glioma-associated oncogene 1 (Gli1). TPB15 shows good anti-tumor activity with low toxicity[1].