STING agonist C11 is a novel cell-permeable STING agonist that activates IFN-dependent signaling processes and induces IFN secretion from human cells; induces transcription and translation of interferon-dependent antiviral genes, induces canonical IRF3 phosphorylation and ISG transcription in a manner that requires STING but not MAVS or TRIF; potently blocks replication of multiple emerging Alphavirus types including Chikungunya, Ross River, Mayaro, and O'nyong'nyong viruses.
GSK2324 (Compd 1c) is a FXR agonist for diabetes study, with an EC50 of 120 nM. GSK2324 exhibits t1/2 values of 84 min (mouse), 170 min (rat), 110 min (beagle) and 120 min (cyno), respectively[1].
Lucideric acid A is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells[1].
RIPK1-IN-9 (example 45), a dihydronaphthyridone compound, is a potent and selective RIPK1 inhibitor. RIPK1-IN-9 inhibits U937 cell (IC50=2 nM) and L929 cell (IC50=1.3 nM)[1].
γ-Lumicolchicine is an inactive analogue of Colchicine (HY-16569)[1]
3',4',5',5,7-Pentamethoxyflavanone is a natural flavonoid compound found in Neoraptua magnifica var. magnifica[1].
Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts[1].
Albaspidin AA displays strong antibacterial activity against the vegetative form of Paenibacillus larvae (P. larvae) (MIC=220 μM)[1].
MMI-0100 is a cell-permeant peptide inhibitor of mitogen activated protein kinase activated protein kinase II (MK2). MMI-0100 reduces intimal hyperplasia ex vivo and in vivo. MMI-0100 suppresses IL-6 expression without effect on IL-8 expression. MMI-0100 suppresses fibrotic processes such as vein graft disease[1].
DPC-AJ1951, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR) , and characterized its activity in ex vivo and in vivo assays of bone resorption[1].
Piperitol is a compound isolated from the Tibetan medicinal plant Lancea tibetica[1].
17α,20β-Dihydroxy-4-pregnen-3-one (17,20β-P) is a maturation-inducing steroid[1].
Kadsuphilin A can be extracted from Kadsura coccinea (Lem.) and has weak antiproliferative activity[1].
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely[1].
5'-O-(4,4'-Dimethoxytrityl)-2'-O-methyl-2-thiouridine is a purine nucleoside analog. 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].
Z-Phe-OBzl is a phenylalanine derivative[1].
[D-Ala2]-Met-Enkephalin, an opioid peptide, is a potent opioid agonist. [D-Ala2]-Met-Enkephalin inhibits ACh-induced and suckling-induced oxytocin (OT) release[1][2].
Aloin(Aloin-A; Barbaloin-A) is a natural antitumor anthraquinone glycoside with iron chelating and non-atherogenic activities.IC50 value:Target:in vitro: Aloin significantly inhibited HUVECs proliferation, migration and tube formation in vitro. suppressed activation of VEGF receptor (VEGFR) 2 and STAT3 phosphorylation in endothelial cells. In addition, the constitutively activated STAT3 protein, and the expression of STAT3-regulated antiapoptotic (Bcl-xL), proliferative (c-Myc), and angiogenic (VEGF) proteins were also down-regulated in response to AL in human SW620 cancer cells [1]. aloin exerted inhibition of cell proliferation, adhesion and invasion abilities of B16-F10 melanoma cells under non-cytotoxic concentrations. Furthermore, aloin induced melanoma cell differentiation through the enhancement of melanogenesis and transglutaminase activity [2].in vivo: Aloin substantially reduced tumor volumes and weight in vivo mouse xenografts, without obviously toxicity [1]. Aloin (10, 30 mg/kg bw) or vehicle was given by gavage to mice after each alcohol administration. Alcohol elevated the serum transaminases alanine aminotransferase, aspartate aminotransferase, total cholesterol and triglyceride levels which were significantly attenuated by the co-administration of aloin (p < 0.05) [3].
Pomaglumetad methionil (LY2140023 hydrate) is an oral methionine prodrug of the potent specific mGlu2/3 receptor agonist LY404039 (HY-50906). Pomaglumetad methionil is well-tolerated and has a distinct safety profile, and can be used to treat schizophrenia[1][2].
Fmoc-Met-OH is a Methionine (HY-13694) derivative[1].
H-L-Photo-Phe-OH is a phenylalanine derivative[1].
Tau-aggregation and neuroinflammation-IN-1 is a potent tau-aggregation and neuroinflammation inhibitor. Tau-aggregation and neuroinflammation-IN-1 exhibits remarkable inhibitory activities against AcPHF6 and full-length tau aggregation. Tau-aggregation and neuroinflammation-IN-1 has a low cytotoxicity and reduced NO release in LPS-stimulated BV2 cells. Tau-aggregation and neuroinflammation-IN-1 can reverse okadaic acid-induced memory impairment in rats[1].
BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD+-competitive PHGDH inhibitor[1].
Eupteleasaponin I is a component of Euptelea polyandra, may has gastroprotective activity[1].
Phosphate dibasic-d2 (sodium) is the deuterium labeled Sodium phosphate dibasic[1].
AC-93253 is a selective, potent SIRT2 inhibitor. AC93253 can inhibit SIRT2 with an IC50 value of 6 μM. AC93253 can be used for the research of tumors[1].
MK196 (MK-196) is an investigational diuretic which has pronounced saluretic activity in the rat and dog as well as both uricosuric and saluretic activity in the chimpanzee.
Herpes virus inhibitor 2 is a herpes virus inhibitor and disrupts herpes virus ribonucleotide reductase quaternary structure. Herpes virus inhibitor 2 inhibits viral replication[1][2].
Octanal-d16 is the deuterium labeled Octanal[1]. Octanal is an aromatic aldehyde, with antioxidant and antimicrobial activities. Octanal shows cytotoxicity against Hela cells[2].
Vitamin A is important for growth and development, for the maintenance of the immune system and good vision. Vitamin A is needed by the retina of the eye in the form of retinal[1].