Boc-N-PEG1-C2-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Rhyncholphylline, an alkaloid isolated from Uncaria, shows potent inhibition of lipopolysaccharide (LPS)-induced NO production in rat primary microglial cells.IC50 value:Target:In vitro: Rhyncholphylline effectively suppresses release of proinflammatory cytokines in LPS-activated microglial cells and the underling molecular mechanism for the inhibition of microglial activation; Attenuated LPS-induced production of proinflammatory cytokines such as TNF-α and IL-1β as well as NO in mouse N9 microglial cells [1]. Rhynchophylline exerts it protective action against ischemia-induced neuronal damage by preventing NMDA, muscarinic M1, and 5-HT2 receptors-mediated neurotoxicity during ischemia [3].In vivo: The neuroprotective effect of rhynchophylline was investigated in a stroke model. Following pMCAO, rhynchophylline treatment not only ameliorated neurological deficits, infarct volume and brain edema, but also increased claudin-5 and BDNF expressions (p < 0.05). Moreover, rhynchophylline could activate PI3K/Akt/mTOR signaling while inhibiting TLRs/NF-κB pathway [2].
4-Bromobenzonitrile-d4 is the deuterium labeled 4-Bromobenzonitrile[1].
Vidofludimus(4SC-101; SC12267) is a novel immunosuppressive drug that inhibits DHODH; inhibits IL-17 secretion in vitro independently of effects on lymphocyte proliferation.IC50 value:Target: DHODH inhibitorin vitro: 4SC-101 is a potent inhibitor of human DHODH, inhibits lymphocyte proliferation, and uniquely blocks phytohemagglutinin-stimulated IL-17 production by lymphocytes [2].in vivo: In vivo Vido treatment alone most effectively reduced macroscopic and histological pathology and the numbers of CD3+ T cells. In contrast, similarly reduced nuclear signal transducer and activator of transcription 3 (STAT3) binding and IL-17 levels were observed from animals treated with Vido alone and Vido + Uri. Vido improves TNBS-induced colonic inflammation by a unique dual mode of action [1]. Oral administration of 4SC-101 effectively improved both chronic DSS and acute TNBS colitis in mice. In these colitis models the overall efficacy profile of 4SC-101 was similar to that of dexamethasone [2].
Acetylcholine is a neurotransmitter that can induce the opening of calcium channels. Target: Calcium Channel; nAChR; mAChRAcetylcholine in vertebrates is the major transmitter at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system. It is generally not used as an administered drug because it is broken down very rapidly by cholinesterases, but it is useful in some ophthalmological applications.Acetylcholine chloride, more commonly referred to as just acetylcholine, is a cholinergic neurotransmitter that can induce the opening of calcium channels, as well as act on nicotinic and muscarinic acetylcholine receptors. Acetylcholine plays an important role at many sites in the central nervous system. The compound has been shown to have ophthalmological uses and can be broken down quickly by choliesterases. Studies show that non-neuronal acetylcholine influences many basic cells functions, such as mitosis, cells differentiation, cytoskeletal organization, and cell to cell contact, among other functions [1-3].
Foscarnet trisodium hexahydrate (Trisodium phosphonatoformate hexahydrate) is a viral DNA polymerase activity inhibitor, leading to reversible suppression of viral replication. Foscarnet trisodium hexahydrate is an antiherpesvirus agent used in cytomegalovirus retinitis[1][2][3].
Mca-Ala-Pro-Lys(Dnp)-OH, a specific ACE2 quenched fluorogenic substrate, can be used to detect ACE2 activity, such as urinary, heart and lung[1][2].
Fludrocortisone, a synthetic mineralocorticoid with anti-inflammatory activity.
MET kinase-IN-4 is an orally active Met kinase inhibitor. MET kinase-IN-4 has potent Met kinase inhibitory activity with an IC50 value of 1.9 nM. MET kinase-IN-4 can be used for the research of cancer[1].
AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.
BET-IN-1 is a bromodomain inhibitor extracted from patent WO/2013024104A1, compound example 2, has a plC50 in the range 6.0 - 7.0.IC50 value: 6.0 - 7.0 (plC50)Target: bromodomain
Moxonidine Hydrochloride is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.Target: I1-RMoxonidine Hydrochloride is a centrally acting antihypertensive agent. Mixed Nischarin (I1 imidazoline receptor) and α2-AR (adrenergic) agonist; displays 40-fold higher affinity for I1 receptors versus α2-adrenoceptors. Moxonidine reduced stimulated NE overflow (log EC50: -6.15 +/- 0.14). AGN192403, a selective ligand at I1-R, had no influence on the dose-response curve of moxonidine (log EC50: -6.01 +/- 0.25) [1]. The hypotensive and bradycardic actions of moxonidine but not clonidine are mediated through imidazoline receptors and are dependent on intact noradrenergic pathways within the RVLM. Furthermore, the noradrenergic innervation may be associated with a 42 kDa imidazoline receptor protein [2].
Ceftibuten(Sch39720) is a third-generation cephalosporin antibiotic.IC50:Target: AntibacterialCeftibuten displayed high activity against Haemophilus influenzae and Branhamella catarrhalis. There was reduced activity against Streptococcus pneumoniae (MIC90 16 mg/l). The protein binding of Ceftibuten was 77% and the primary target site PBP 3. A high degree of stability to beta-lactamase hydrolysis was observed. [1]
Racecadotril (acetorphan), a potent enkephalinase inhibitor (IC50= 4.5 uM), protects endogenous enkephalins from degradation. IC50 value: 4.5 uMTarget: EnkephalinaseRacecadotril is a peripherally acting enkephalinase inhibitor with an IC50 of 4.5 uM. Unlike other medications used to treat diarrhea, which reduce intestinal motility, Racecadotril has an antisecretory effect-it reduces the secretion of water and electrolytes into the intestine. A small randomized controlled trial found Racecadotril to significantly reduce the duration and volume of watery diarrhea in children when given as an adjunct to oral rehydration therapy.
L 640035 is athromboxaneantagonist[1].
BPU-11 is a hyperpolarization-activated cyclic nucleotide-gated (HCN) C-linker pocket (CLP) HCN4 CLP ligand. BPU-11 can be used for the research of congenital immune disease[1].
AA-Z-YVAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor with anti-inflammatory and anti-tumor activities.
GW 833972A is a selective CB2 receptor agonist. GW 833972A inhibits induced nerve depolarization and citric acid-induced cough in animal models[1].
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively[1].
Resatorvid (TAK-242) is a potent TLR4 signaling inhibitor which selectively inhibits the TLR4-mediated production of cytokines and nitric oxide.
LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells. LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively[1].
Equisetin is an N-methylserine-derived acyl tetramic acid isolated from a terrestrial fungus Fusarium equiseti NRRL 5537[1]. Equisetin is a tetramate-containing natural product with antibiotic and cytotoxic activity[2]. Equisetin inhibits the growth of Gram-positive bacteria and HIV-1 integrase activity but shows no activity against Gram-negative bacteria[3]. Equisetin is a Quorum-sensing inhibitor (QSI) that attenuates QS-regulated virulence phenotypes in P. aeruginosa without affecting the growth of bacterias, serves as a leading compound for the treatment of P. aeruginosa infections[4].
Guangxitoxin 1E is a potent and selective blocker of KV2.1 and KV2.2 channels. Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM. KV2 channels underlie delayed-rectifier potassium currents in various neurons[1][2].
N-Dodecyl-N,N-dimethyldodecan-1-aminium-d5 (bromide) is the deuterium labeled N-Dodecyl-N,N-dimethyldodecan-1-aminium bromide[1].
Methyl arachidate (Methyl eicosanoate), a natural compound, is a leukotriene A4 hydrolase (LTA4H) inhibitor[1].
1-Dodecylimidazole (N-Dodecylimidazole) is a lysosomotropic detergent and a cytotoxic agent. 1-Dodecylimidazole causes cell death by its acid-dependent accumulation in lysosomes, disruption of the lysosomal membrane, and releaseof cysteine proteases into the cytoplasm. 1-Dodecylimidazole has hypocholesterolaemic activity and broad-spectrum antifungal activity[1][2][3].
CMLD012073 is an amidino-rocaglates and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012073 against NIH/3T3 cells with an IC50 of 10 nM. CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A)[1].
(S)-3-((tert-Butoxycarbonyl)amino)-3-(pyridin-3-yl)propanoic acid is an alanine derivative[1].
G0 N-glycan-Asn is a glycopeptide. G0 N-glycan-Asn can be used for various biochemical studies[1].
(4S)-4-Phenyl-L-proline is a proline derivative[1].