12-Hydroxyjasmonic acidis is a COI1-JAZ-independent activator of leaf-closing movement in Samanea saman[1].
Norflurazon (SAN 9789) is a bleaching herbicide. Norflurazon can block carotenoid biosynthesis by inhibiting phytoene desaturase activity[1].
Triptoquinone H is a class of natural product isolated from traditional Chinese medicine Tripterygium hypoglaucu. Triptoquinone H has strong cytotoxic, immunomodulatory and anti-inflammatory activities. Triptoquinone H can be used for cancer or inflammatory diseases research[1].
Propargyl-PEG4-thiol is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
SKF 38393 hydrochloride is a D1 agonist with IC50 of 110 nM.IC50 value: 110 nM [1]Target: D1 agonistin vitroL SKF 38393 hydrochloride is a benzazepine selective agonist of the D1DR (dopamine D1 receptor). Agonism of the D1DR by SKF 38393 is correlated to induced desynchronization of electroencephalographic activity in rats. SKF 38393 is also reported to demonstrate agonism of the serotonin SR-2C (5-HT1C receptor). SKF 38393 HCl is an activator of D5DR. SKF 38393 is a synthetic compound of the benzazepine chemical class which acts as a selective D1/D5 receptor partial agonist. It has stimulant and anorectic effects. SKF-38393 enhances the frequency of mEPSCs in a concentration-dependent manner. SKF-38393 enhances the frequency of mEPSCs in a concentration-dependent manner. [2]
Anthragallol 1,2-dimethyl ether (compound 11) can be isolated from O. umbellata. Anthragallol 1,2-dimethyl ether has cytotoxicity, with IC50 values of 5.9 and 8.8 μg/ml against A549 cells and MDA-MB-231 cells, respectively[1].
The amine-reactive 5-TAMRA, SE and its conjugates yield bright, pH-insensitive orange-red fluorescence (approximate excitation/emission maxima ~546/579) with good photostability.
Edicotinib is a selective and orally available colony-stimulating factor-1 (CSF-1) receptor inhibitor, and has entered phase IIA clinical trial to study rheumatoid arthritis (RA) despite disease.
Spectinomycin is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin is also a noncompetitive inhibitor of td intron RNA[1][2][3][4][5].
Gefitinib impurity 5 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
EMD638683 S-Form is the S-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
LCMV-derived p13 epitope is a biological active peptide. (An H-2Db restricted epitope, this peptide is amino acids 61 to 80 fragment of the lymphocytic choriomeningitis virus (LCMV) pre-glycoprotein polyprotein GP complex. LCMV has been routinely used for the study of adaptive immune responses to viral infection.)
3-Methyloctane-d20 is the deuterium labeled 3-Methyloctane[1].
Dalbavancin is a lipoglycopeptide antibiotic agent that is active against gram-positive pathogens.
Methyl β-D-glucopyranoside-d1 is the deuterium labeled Methyl β-D-glucopyranoside. Methyl β-D-glucopyranoside is used to synthesize natural glycophenolics via enzymatic caffeoylation[1][2].
Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells[1].
L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice[1][2].
Fmoc-MeSer(Bzl)-OH is a serine derivative[1].
WEHI-345 (analog) is a Src inhibitor, extracted from patent WO/2012003544A1, compound example 71.Target:SrcWEHI-345 (analog) is a protein kinase inhibitor. A family of proto-oncogenic TPKs referred to herein as SFKs (Src family kinases) have provided researchers with a better understanding of the mechanism of cancer as a disease state where normally healthy cellular signalling is disrupted.
Angeloylbinankadsurin A (compound 7) is an anti-rheumatoid arthritis (RA) agent that can be isolated from EtOAc and CH2Cl2 extracts of Black Tiger Beard. Angeloylbinankadsurin A exhibits inhibitory activity on RA-FLS cells (IC50=11.70 μM). Angeloylbinankadsurin A is slightly toxic to human cancer cell lines (Hela and BGC-823) (IC50=19.9 μM, 21.93 μM)[1].
Pumaprazole is a reversible proton pump antagonist.
Trichodesmine is a dehydropyrrolizidine alkaloid. Trichodesmine can produces hepatotoxicty, pneumo- and neurotoxicity in vivo[1][2].
Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
Astragaloside A is one of the major active constituents of Astragalus membranaceus in Traditional Chinese Medicine; has been widely used to treat ischemic diseases.IC50 value: Target: in vitro: AS-IV treatment promotes umbilical vein endothelial cells (HUVEC) proliferation, migration, and tube formation. AS-IV treatment also activates JAK2/STAT3 and ERK1/2 signaling pathways, and up-regulates endothelial nitric oxide synthase (eNOS) expression and nitric oxide (NO) production [1]. Administration of astragaloside IV (16, 32, and 64 μM) 1 h prior to lipopolysaccharide stimulation dose-dependently attenuated cardiac hypertrophy induced by lipopolysaccharide. Further studies demonstrated that astragaloside IV inhibited the increment of the resting intracellular free Ca2+, and its effect was similar to verapamil [2]. ASI could inhibit cells apoptosis induced by high glucose (25mmol/L) in dose-dependent and time-dependent manners. ASI also inhibited high glucose-induced expression of TGF-β1 and activation of p38 MAPK pathway at the protein level. Furthermore, ASI increased HGF production in human tubular epithelial cells [3].in vivo: the growth of tumor was suppressed by AS-IV treatment in vivo. AS-IV also could down-regulate regulatory T cells (Tregs) and up-regulate cytotoxic T lymphocytes (CTLs) in vivo and in vitro[4]. As an in vivo model, mice subjected to unilateral ureteral obstruction (UUO) were administered AS-IV (20 mg/kg) by intraperitoneal injection for 7 days. AS-IV significantly alleviated renal mass loss and reduced the expression of α-smooth muscle actin, fibronectin, and collagen IV both in vitro and in vivo [5].
Arteminin is a coumarin that can be found in Artemisia apiacea[1].
2-(4-Nonylphenoxy)acetic acid-d2 is the deuterium labeled 2-(4-Nonylphenoxy)acetic acid[1].
Apatinib is a highly selective VEGFR2 inhibitor with an IC50 of 1 nM. Apatinib also potently suppresses the activities of Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively.
Casein Kinase II Receptor Peptide is a substrate for casein kinase II with an Km value of 500 µM. Casein Kinase II Substrate can be used for measure casein kinase II activity in crude enzyme preparations[1].
N2-Phenoxyacetylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].