Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis[1][2][3].
2-Hexylthiophene is an extremely weak basic heteroaromatic compound. 2-Hexylthiophene can be used to modify and improve the molar absorption coefficient of ruthenium sensitizer[1]
Fmoc-His(Mtt)-OH is a histidine derivative protected by Fmoc, can be used for the synthesis of drugs or other compounds[1].
MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively[1]. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells[2].
SMS2-IN-2 is a potent, highly selective and orally active sphingomyelin synthase 2 (SMS2) inhibitor, with IC50s of 100 nM and 56 μM for SMS2 and SMS1, respectively. Anti-chronic inflammatory activity[1].
HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells[1].
9-(2’-Deoxy-2’-fluoro-β-D-arabinofuranosyl)-9H-purine is a purine nucleoside analogue. 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].
Formosanin C is a diosgenin saponin isolated from Paris formosana Hayata and an immunomodulator with antitumor activity. Formosanin C induces apoptosis[1][2].
Saponin CP6 is a triterpenoid compound from the roots of Clematis grata[1].
U-69593 is a potent and selective κ1-opioid receptor agonist[1]. U-69593 attenuates cocaine-induced behavioral sensitization in the rat[2]. U-69593 reduces anxiety and enhances spontaneous alternation memory in mice[3]. U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum[4].
LY 81067 is a new anticonvulsive compound that effectively protects against pentylenetetrazole- and picrotoxin-induced convulsions in mice. It exerts its anticonvulsant effects by binding to or near picrotoxin binding sites.
Dehydrovomifoliol is a AKT/mTOR dual inhibitor. Dehydrovomifoliol reduces lipid accumulation and lipogenesis by inhibiting the AKT/mTOR signaling pathway. Dehydrovomifoliol is used in nonalcoholic fatty liver disease research (NAFLD) .
Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist.
Kushenol X, a flavonoid compound isolated from the roots of Sophora flavescens. Kushenol X is a potent β-glucuronidase and human carboxylesterase 2 (hCE2) inhibitor with IC50s of 2.07 μM and 3.05 μM, respectively[1][2].
LYG-202, a flavonoid, has potent anti-angiogenic and antitumor activity. LYG-202 inhibits VEGF-stimulated HUVEC migration and tube formation. LYG-202 induces cancer cell apoptosis[1][2].
Methyl N,O-bis(tert-butoxycarbonyl)-L-serinate is a serine derivative[1].
Natamycin (pimaricin) is an antifungal macrolide polyene that binds to cell membrane sterols.Target: AntifungalNatamycin (INN), also known as pimaricin and sometimes sold as Natacyn, is a naturally occurring antifungal agent produced during fermentation by the bacterium Streptomyces natalensis, commonly found in soil. Natamycin has a very low solubility in water; however, natamycin is effective at very low levels. There is an MIC (minimum inhibitory concentration) of less than 10 ppm for most molds. Natamycin is classified as a macrolide polyene antifungal and, as a drug, is used to treat fungal keratitis. It is especially effective against Aspergillus and Fusarium corneal infections. Other common members of the polyene macrolide antifungal family are amphotericin B, nystatin, and filipin. Natamycin is also used in the food industry as a natural preservative.Natamycin is used to treat fungal infections, including Candida, Aspergillus, Cephalosporium, Fusarium and Penicillium. It is applied as a cream, in eyedrops, or (for oral infections) in a lozenge. Natamycin shows negligible absorption into the body when administered in these ways. When taken orally, little or none is absorbed from the gastrointestinal tract, making it inappropriate for systemic infections.
IL-17 modulator 8 (compound 286) is an orally active modulator of IL-17. IL-17 modulator 8 significantly reduces IL-6, IFN-γ, and edema. IL-17 modulator 8 can used in study arthritis[1].
Mezilamine is a potent antidopaminergic agent. Mezilamine induces a concentration dependent increase in the electrically stimulated overflow of 3H-noradrenaline from rat cortical slices, without affecting the basal overflow. Mezilamine acts as a presynaptic α-adrenoceptor antagonist and a postsynaptic α-adrenoceptor agonist[1].
GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
m-PEG8-succinimidyl carbonate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
10-Deacetyltaxol (10-Deacetylpaclitaxel) is a taxane derivative isolated from Taxus wallichiana Zucc[1]. 10-Deacetyltaxol (10-Deacetylpaclitaxel) promotes the polymerization of tubulin and to inhibit the depolymerization of microtubules induced by cold or by calcium ions in vitro[2]. 10-Deacetyltaxol (10-Deacetylpaclitaxel) exhibits cytotoxicity in human glial and neuroblastoma cell-lines[3].
Arrhythmias-Targeting Compound 1 is used in the research of arrhythmias, extracted from patent WO 2001028992 A2.
Fmoc-NH-PEG3-C2-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Thalidomide-5-O-C3-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C3-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].
HO-PEG11-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
1-(3,4-Dimethoxyphenyl)ethanone-d3 is the deuterium labeled 1-(3,4-Dimethoxyphenyl)ethanone[1].
Pemirolast is an orally active antiallergic agent. Pemirolast attenuates paclitaxel hypersensitivity reactions, can be used for bronchial asthma and conjunctivitis research[1]-[5].
AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.
HER2-IN-14 (Compound 34) is an HER2 inhibitor with an IC50 of 18 nM. HER2-IN-14 also inhibits wt-EGFR with an IC50 of 6.3 μM[1].