Peimisine (Ebeiensine) hydrochloride non-competitively antagonizes tracheal smooth muscle muscarinic M receptor and inhibits smooth muscle contraction caused by Ach. Peimisine hydrochloride excits β-receptor, restrains the release of internal calcium, and promotes to releaseing NO in order to relax tracheal smooth muscle and relieve asthma[1].
PC Alkyne-PEG4-NHS ester is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
N-(Azide-PEG3)-N'-(PEG4-acid)-Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
AS6 is an ABA-induced PYL-PP2C interaction antagonist in a dose-dependent manner.
Quercetin (dihydrate), a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively[1].
Indeno[1,2,3-cd]pyrene-d12 is the deuterium labeled Indeno[1,2,3-cd]pyrene[1].
4-Methylumbelliferyl β-cellotrioside, a chromogenic substrate for β-glycosidases, is a cellulose fluorescent derivative[1].
Nitrofurantoin is an antibiotic usually used to treat urinary tract infections.
Siraitic Acid A is a cucurbitane triterpenoid isolated from the root of S. grosvenori [1].
Sorafenib tosylate is a potent multikinase inhibitor, with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
4-Methyl-2-oxo-2H-1-benzopyran-7-yl decanoate is a fluorogenic substrate used to follow the hydrolytic activity of carboxylesterases[1].
Methyl vanillate glucoside is a secondary metabolite thatcan be isolated from Lycium schweinfurthii[1].
Regaloside A, a phenylpropanoid, shows significant DPPH radical scavenging activity of 58.0% at 160 ppm. Regaloside A has anti-inflammatory activity[1].
Prepro-ANF (56-92), human is a human atrial natriuretic factor precursor. Prepro-ANF (56-92), human is also a Guanylate Cyclase activator that enhances particulate Guanylate Cyclase activity in the renal membrane and renal unit[1].
Gentamicin sulfate, an aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. It inhibits DNase I with an IC50 of 0.57 mM.
DS28120313 (compound 32) is an orally hepcidin production inhibitor with an IC50 of 0.093 μM[1].
IOWH-032 is a novel and potent CFTR inhibitor (IC50=1.01 uM) in T84 and CHO-CFTR cell based assays.IC50 value: 1.01 uM (CHO-CFTR FLIPR) [1]Target: CFTRProfiling of iOWH032 showed it to be a CFTR inhibitor in T84 and CHO-CFTR cell based assays. It also demonstrated statistical significant inhibition at both 100 g & 10 g doses in the mouse closed-loop model. iOWH032 was further profiled in a cecetomized rat model. iOWH032 reduced the fecal output index by ~70%, compared to vehicle (choleratoxin), up to 8 hours after a single 5 mg/kg po dose.
LXS196 is a potent and orally active protein kinase C (PKC) inhibitor under Phase I clinical trials for the treatment of uveal melanoma.
4-Methylbenzenesulfonhydrazide-d3 is the deuterium labeled 4-Methylbenzenesulfonhydrazide[1].
EDI048 (compound 1.16) is an orally active Cryptosporidium PI4K inhibitor for the research of cryptosporidiosis[1].
Goniotriol(compound 2) is a styrylpyronethat can be found in Goniothalamus amuyon. Goniotriolshows cytotoxicity[1].
2'-Ethyl Simvastatin (compound 6) is a Mevinolin analog, with HMG-CoA reductase inhibition[1].
MK-8318 is potent and selective CRTh2 receptor antagonist with a Ki of 5.0 nM.
Isotachioside is a aromatic glucoside that can be found in Berchemia racemosa[1].
Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with an IC50 of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with an IC50 of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies[1][2].
PAT-1251 is a potent, selective and oral Lysyl Oxidase-Like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively); PAT-1251 has entered clinical development with the potential to treat a number of fibrotic diseases.
Dihydrobaicalin is a flavonoid glycoside, which can be isolated from American skullcap (Scutellaria lateriflora L.)[1].
Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.IC50 Value: 0.14 μM(EC50 for 5-HT4 receptor) [1]; 9.8 μM (Kv4.3) [2]Target: 5-HT4 Receptorin vitro: Cisapride showed higher inhibitory effects on a hERG current, as indicated by its IC50 of 9.4 × 10-9 M [1]. cisapride on cloned Kv4.3 channels stably expressed in Chinese hamster ovary cells were investigated using the whole-cell patch-clamp technique. Cisapride inhibited Kv4.3 in a concentration-dependent manner with IC50 values of 9.8 uM [2].in vivo: Cisapride (1 mg/kg i.v.), when administered 10 min after the start of GR113808 infusion, did not stimulate either antral or colonic motor activity under treatment with GR113808. The enhanced antral or colonic motor activity induced by these drugs was antagonized by treatment with GR113808 in dogs [3]. cisapride could not bring about more colitis damages through 5HT(4) receptors. Based on the present study further researches are required for investigating the exact roles of 5HT(4) receptors in the pathogenesis of ulcerative colitis[4].Toxicity: cardiac arrythmies
GSK805 is a potent, orally bioavailable RORγγ Inhibitor with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.
RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC50 of 119 nM[1].