ELQ-300 is a potent and orally bioavailable antimalarial agent, acts as an inhibitor of the reductive (Qi) site of the cytochrome bc1 complex (cyt bc1). 了解更多
QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively). 了解更多
Hypotaurine (2-aminoethanesulfinic acid), an intermediate in taurine biosynthesis from cysteine in astrocytes, is an endogenous inhibitory amino acid of the glycine receptor. 了解更多
TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. 了解更多
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. 了解更多
Indotecan (LMP-400) is a potent topoisomerase 1(Top1) inhibitor with IC50 values of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. 了解更多
Renata Santos, .et al. Generation of inflammation-responsive astrocytes from glial progenitors derived from human pluripotent stem cells, STAR Protoc, 2022, Mar 17;3(2):101261 PMID: 35313707
Chlorantraniliprole is an insecticide that potently and selectively activates insect ryanodine receptor, with EC50s of 40 nM and 50 nM for Drosophila melanogaster and H. virescens ryanodine receptor, and ?300-fold more potent than that in the mouse myoblast cell line, C2C12 (EC50, 14 μM). 了解更多
SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues. 了解更多
PF-4191834 is a novel, potent and selective non-redox 5-lipoxygenase inhibitor effective in inflammation and pain with an IC50=229 nM. displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes. 了解更多
JAK3-IN-2 is a potent and highly selective JAK3 inhibitor with IC50 of 0.15 nM. dispalys >4,300-fold selectivity over JAK1, JAK2 and TYK2, and other kinases BMX, EGFR, ITK and BTK; blocks cytokine signaling through JAK3, but not through other JAK family enzymes; inhibits IL-7 induced pSTAT5 in CD3+, CD8+ T cells with IC50 of 280 nM; sufficiently blocks the development of inflammation in a rat model of rheumatoid arthritis, while sparing hematopoiesis. 了解更多
Oxprenolol is an orally bioavailable β-adrenergic receptor (β-AR) antagonist (Ki = 7.10 nM in a radioligand binding assay using rat heart tissue). It is non-selective and inhibits both β1- and β2-ARs (Kds = 2.09 and 1.35 nM in isolated rat heart and uterus, respectively). Oxprenolol is selective for β-ARs over serotonin (5-HT) receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively), but it binds to 5-HT1A receptors in rat hippocampus and 5-HT1B in rat striatum (Kis = 94.2 and 642 nM, respectively). 了解更多
Hongwei Liu, .et al. Evidence for the plant recruitment of beneficial microbes to suppress soil-borne pathogens, New Phytol, 2020, Oct 31 PMID: 33131088
Pholwat S, .et al. Genotypic antimicrobial resistance assays for use on E. coli isolates and stool specimens, PLoS One, 2019, May 10;14(5):e0216747 PMID: 31075137
Meikle V, .et al. A protein complex from human milk enhances the activity of antibiotics and drugs against Mycobacterium tuberculosis, Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
Weizhen Chen, .et al. An improved osseointegration of metal implants by pitavastatin loaded multilayer films with osteogenic and angiogenic properties, Biomaterials, 2021, 280:121260 PMID: 34823885
Karis Tutuska, .et al. Statin as anti-cancer therapy in autochthonous T-lymphomas expressing stabilized gain-of-function mutant p53 proteins, Cell Death Dis, 2020, Apr; 11(4): 274 PMID: 32332697
D Jarmuzek, .et al. Phototransformations of pitavastatin - The inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase, J Photochem Photobiol A Chem, 2019, November
Marwan Ibrahim Abdullah, .et al. Inhibition of the mevalonate pathway augments the activity of pitavastatin against ovarian cancer cells, Sci Rep, 2017, 7: 8090 PMID: 28808351
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