3-Methyladenine is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K.
Bromodomain inhibitor-9 is a Bromodomains inhibitor that selectively inhibits BRD4-1 (Kd: 12 nM). Bromodomain inhibitor-9 can be used in the research of diseases or conditions associated with systemic or tissue inflammation, lipid metabolism, fibrosis or chronic autoimmune diseases[1].
(Tyr0)-Urocortin, rat is a high-affinity agonist of corticotropin-releasing factor receptor type 1 (CRF-R1) and type 2 (CRF-R2). (Tyr0)-Urocortin, rat shows inhibitory binding constants (Ki) of 1-2 nM[1].
Homomangiferin, isolated from the leaves of M. indica L., is mangiferin monomethyl ether. Homomangiferin has important medicinal properties and is widely used to relieve many symptoms, for example coughing and asthma[1].
Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM.Target: ACERamipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM [1]. Ramipril enhances the activity of ACE-associated CK2 and the phosphorylation of ACE Ser1270 in cultured endothelial cells, but is unable to activate JNK or stimulate the nuclear accumulation of c-Jun in endothelial cells expressing a S1270A ACE mutant or in ACE-deficient cells. Prolonged Ramipril treatment increases ACE expression in primary cultures of human endothelial cells and in vivo (mouse lung), which can be prevented by pretreatment with the JNK inhibitor SP600125 [2].Chronic in vivo administration of Ramipril to rats at a dosage that has similar hypotensive effects in vitro HUVECs significantly reduces the rate of LPS-induced apoptosis compared to the other ACE inhibitors, which contrasts with the apoptosis effect in vitro [3]. Ramipril inhibits systolic blood pressure (SBP) with IC50 of 1.97 mg/kg in spontaneously hypertensive rats (SHR). When in combination with AT1-receptor blockade by candesartan-cilexetil increases SBP reduction synergistically rather than additively [4].
Macrosphelide A is a macrolide antibiotic. Macrosphelide A inhibits growth of some ascomycetes, basidiomycetes, oomycetes and all four Gram-positive bacteria tested, including the medically important Staphylococcus aureus with a MIC of ≤500 μg/mL[1].
Oxetorone fumarate is a non-selective, orally active serotonin antagonist. Oxetorone fumarate is an antimigraine agent[1].
Hydroxy-PEG2-(CH2)2-Boc is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG2-(CH2)2-Boc is extracted from patent WO2004008101A2 (compound 196)[1].
Spicamycin, an adenine nucleoside antibiotic with antifungal and antitumor activities. Spicamycin is also a potent inducer of differentiation of myeloid leukemia cells. Spicamycin induces apoptosis in NB4 cells via down-regulation of Bcl-2 expression and modulation of PML protein[1][2].
LY 227942-d3 oxalate is the deuterium labeled LY 227942[1].
Propacetamol is a water-soluble acetaminophen precursor drug, which can be administered via non intestinal route. It is an analgesic used to treat postoperative pain, acute trauma and gastrointestinal disorders[1].
Methyl Ganoderic acid B is a triterpenoid, that can be isolated from Ganoderma lucidum. Methyl Ganoderic acid B has nerve growth factor-like neuronal survival-promoting effects[1].
ΧΜΤ-1519 conjugate-1 (compound 31) is a linker for the HER-2 monoclonal antibody XMT-1519, which can be used to synthesize ADC and increase anti-tumor activity[1].
DDX3-IN-1 (Compound 16f) is a DEAD-box polypeptide 3 (DDX3) inhibitor with CC50s of 50 and 36 μM for HIV and HCV, respectively. Antiviral activity[1].
Sofigatran (MCC-977) is an orally active factor IIa (thrombin) inhibitor, acts as an anticoagulant. Sofigatran is used for the research of cardiovascular disease[1].
Rutacridone is an alkaloid that can be cultured from Ruta graveolens L. strain R-19[1].
Leucine dehydrogenase can be purified from Bacillus spheroides. Leucine dehydrogenase catalyzed the oxidative deamination of L-leucine, L-valine, L-isoleucine, L-norvaline, L-alpha-aminobutyrate, and L-norleucine, and the reductive amination of their keto analogues[1].
PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple drug resistance (MDR) solid tumor model when given in combination with Doxorubicin[1].
2-Bromo-N,N,N-trimethylethanaminium bromide is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
AL-34662 is a selective 5-HT2A receptoragonist (IC50: 0.77 nM and 1.5 nM for rat and human 5-HT2 receptor). AL-34662 is also a weak α-1D adrenergic agonist activity (EC50:0.4 μM). AL-34662 is an ocular hypotensive agent[1][2].
Fenbendazole sulfone (Oxfendazole sulfone;FBZ-SO2) is a minor metabolite of Fenbendazole in plasma and is a benzimidazole anthelmintic agent[1][2].
10-Cl-BBQ is a high affinity AhR ligand with immunosuppressive activity. 10-Cl-BBQ promotes cytosol to nuclear translocation of AhR and activates the AhR-regulated reporter gene at nanomolar concentrations[1][2].
Z1078601926 is an allosterical inhibitor of human dopamine transporter (hDAT). Z1078601926 has synergistic effect with Nomifensine (HY-B1110)[1].
RyRs activator 4 (compound B18) is an insect ryanodine receptor activator. RyRs activator 4 has a larvicidal activity of Mythimna separata with an LC50 value of 1.32 mg/L[1].
Antiarrhythmic peptide (cattle atrium), a hexapeptide, shows a protective effect against experimental drug induced arrhythmias[1].
Metronidazole acetic acid is a metabolite of Metronidazole with mutagenic activity in bacteria. Metronidazole is a nitroimidazole antibiotic, amebicide, and antiprotozoal agent used particularly for anaerobic bacteria and protozoa[1][2][3].
E3 Ligase Ligand-Linker Conjugate 1 incorporates a ligand for the E3 ubiquitin ligase, and a PROTAC linker, which bring together target protein and ubiquitinating machinery.
Liranaftate is a squalene epoxidase inhibitor with anti-fungicidal activities. Target: AntifungalLiranaftate showed excellent fungistatic activity against the conidia of T. rubrum. For each of these agents, the MIC after 14 days of contact was 0.009 g/ml. The liranaftate-induced decrease in the MCC occurred from 9 days onwards; MCC at 14 days was 0.039 g/ml [1]. In time-kill studies, liranaftate showed the greatest decrease to a below detection limit in viable counts of T rubrum. The degree of killing of the strain by amorolfine was not greater than that seen by liranaftate, and little reduction of the viable counts by luliconazole and ketoconazole was observed irrespective of concentrations of the agents [2].
Bersiporocin is a prolyl-tRNA synthetase inhibitor. Bersiporocin has an IC50 of ≤100 nM for phosphoribosylpyrophosphate synthetase (PRS). Bersiporocin can be used for the research of antifibrotic[1][2].
Ibutilide (U70226E free base), an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells[1].