Angelicone (Glabralactone) is a coumarin. Angelicone can be isolated from Fatoua villosa[1].
6-Chloro-9-(2-O-methyl-beta-D-ribofuranosyl)-9H-purin-2-amine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
1,4-Dichloro 6-carboxytetramethylrhodamine is a fluorescence labeling agent (Ex=541 nm, Em=568 nm).
Histone H4 (2-21) is the core histones associated with chromatinization of herpes simplex virus 1 (HSV-1) genomes[1].
LL-37 amide is a positively charged antimicrobial peptide. LL-37 amide has anticancer activity and can be used for cancer research[1][2].
Propargyl-PEG6-N3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
5-n-Heneicosylresorcinol (5-Heneicosylresorcinol) is an active n-alkyl(enyl)resorcinols (AR) occurring in cereal products from Colombia. Antifungal activity[1].
GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively[1].
SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus[1].
Camstatin, a functionally active 25-residue fragment of PEP-19's IQ motif, binds calmodulin and inhibits neuronal nitric oxide (NO) synthase[1].
Muzolimine (BAY-g 282) is a slow and long lasting diuresis agent. Muzolimine produces a diuresis in the loop of Henle and also shows anti-hypertensive effects. Muzolimine can be used for the research of cardiovascular disease[1][2].
4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties[1][2][3].
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].
Oxetorone fumarate is a non-selective, orally active serotonin antagonist. Oxetorone fumarate is an antimigraine agent[1].
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].
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].
N-Acetylmuramic acid-alkyne is a derivative of N-acetylmuramic acid (NAM) component of bacterial peptidoglycans. N-Acetylmuramic acid-alkyne incorporates into bacterial peptidoglycans during biosynthesis. N-Acetylmuramic acid-alkyne can be used for fluorescent labeling of peptidoglycans when 'click'-conjugated to a fluorescent dye.
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].
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].
LY 227942-d3 oxalate is the deuterium labeled LY 227942[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].
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].
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].
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].