Aldose reductase-IN-1 is a inhibitor of aldose reductase with IC50 of 28.9 pM.IC50 value: 28.9 pMTarget: aldose reductaseDetailed information please refer to WO2014113380 A1 and US20130225592.
E3 ligase Ligand 22 (compound 139) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway[1].
Cinitapride monotartrate is a 5-HT1A and 5-HT4 agonist. Cinitapride monotartrate is also a 5-HT2A and D2 antagonist. Cinitapride monotartrate can be used for the research of functional dyspepsia[1][2].
Antibacterial agent 65 is a potential antimicrobial and antioxidant agent.
D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro[1].
Palmitic acid-d2-3 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
(D-Trp6)-LHRH (2-10) is a biologically active peptide.
Lefamulin (BC-3781) is an orally active antibiotic. Lefamulin inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome. Lefamulin has anti-inflammatory activity. Lefamulin can be used in the research of bacterial infections, such as bacterial pneumonia[1].
CB2R probe 1 is a safe and green CB2R (cannabinoid 2 receptor) fluorescent probe with an Ki of 130 nM. CB2R probe 1 shows low cytotoxicity in cancer cells[1].
Manassantin B (compound 6) is a kind of lignan. Manassantin B can be isolated from the ethyl acetate extract of the roots of Saururus chinensis. Manassantin B has cytotoxicities against HT-29 with an IC50 value of 12 μM[1].
PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively), PF-431396 has a Kd value of 445 nM for BRD4.IC50 value: 2 nM (FAK); 11 nM (PYK2); 445 nM (KD for BRD4) [1] [2]Target: FAK; PYK2; BRD4in vitro: PF-431396 is a potent and highly selective pyrimidine-based inhibitor of both Pyk2 and FAK, Consistent with the idea that the tyrosine phosphorylation of Pyk2 and FAK involves an initial autophosphorylation or transphosphorylation step, treating A20 cells with PF-431396 blocked anti-Ig-induced tyrosine phosphorylation of Pyk2 and FAK when the cells were stimulated in suspension when they were stimulated on ECM [3]. Nanomolar affinities were also determined for PF-431396 (Kd = 445 ± 42 nM) and for the PIM inhibitor (Kd = 565 ± 63 nM) [2].
Daclatasvir-d6 is deuterium labeled Daclatasvir. Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].
C12 NBD galactosylceramide, fluorescent dye, is a biologically active derivative of galactosylceramide that is tagged with a fluorescent C12 nitrobenzoxadiazole (C12 NBD) group. C12 NBD galactosylceramide can be used for the research of imaging[1].
3,4',5-Trichloro-1,1'-biphenyl-d4 is the deuterium labeled 3,4',5-Trichloro-1,1'-biphenyl[1].
ANEB-001 is an orally active CB1 inhibitor, can be used to research acute cannabinoid intoxication[1].
Picroside III is an iridoid glycoside isolated from Picrorhiza scrophulariiflora (PS), a traditional Chinese medicine[1].
Rebamipide is an inducer of endogenous prostaglandin and a oxygen-derived free radical scavenger.Target: OthersRebamipide is the first anti-gastric ulcer and antigastritis drug that not only increases endogenous prostaglandin in gastric mucosa but also scavenges oxygen-derived free radicals and inhibits their production. The inhibitory effect of rebamipide on lipid peroxidation induced by a free radical initiator was also demonstrated by the in vitro system using rat gastric mucosal homogenates. These data indicate that rebamipide offers a potential for protection against reactive oxygen- and activated neutrophil-associated gastric mucosal injury by scavenging hydroxyl radical and inhibiting neutrophil activation or lipid peroxidation [1]. Rebamipide can contribute to the management of patients who are taking NSAIDs or are infected with H. pylori. Rebamipide may enhance eradication of H. pylori-infection using standard eradication therapy [2]. Rebamipide is beneficial for obtaining a better quality of ulcer healing and reduction of future ulcer relapse [3].
ML216(CID-49852229) is a potent inhibitor of the DNA unwinding activity of BLM helicase; showing similar IC50s of 3.0 and 0.97 μM for full length BLM and BLM636–1298 respectively.IC50 value: 3.0/0.97 uM(Full length/636–1298 BLM)Target: BLM helicase inhibitorML216 shows cell-based activity, and can induce sister chromatid exchanges, enhance to the toxicity of aphidicolin and exert anti-proliferative activity in cells expressing BLM, but not in those lacking BLM.
Carboprost (15(S)-15-Methyl Prostaglandin F2α) is a metabolically stable synthetic analog of prostaglandin F2α. Carboprost stimulates uterine contractions and induces abortion. Carboprost is used for postpartum hemorrhage due to uterine atony and for the termination of pregnancy in the second trimester[1][2].
(R)-IDHP is an isomer of IDHP, a salvia metabolite that exerts vasorelaxant effects by inhibiting Ca2+ release and Ca2+ inward flow in voltage-dependent and receptor-operated calcium channels in vascular smooth muscle cells. IDHP is used in studies of cardiovascular disease[1].
Octylbenzene-d5 is the deuterium labeled Octylbenzene[1].
6-CFDA is fluorescent polyanionic probe, and its derivatives such as 2′,7′-bis (2-carboxyethyl)-5(6)-carboxyfluorescein are used to measure changes in intracellular pH (pHi) and processes such as dendrimer aggregation and absorption.
Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of 5-HT1A with an IC50 of 370 nM.
BTZ043 Racemate is the racemate of BTZ043, BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), and the antimicrobial activity of BTZ043 is more potent than BTZ043 Racemate.
Tetrasodium,4-(1,10-phenanthrolin-4-yl)benzenesulfonate,ruthenium((II)) is a luminescent indicator dye[1].
Celangulin XIX is a insecticidal that can be isolated from Celastrus angulatu. Celangulin XIX has strong insecticidal activity against Mythimna separate with an ED50 of 73.3 μg/g[1].
T16A(inh)-C01 is an inhibitor of TMEM16A (ANO1). T16A(inh)-C01 blocks chloride channel mediated by ANO1 with an IC50 of 8.4 μM, without interfering with calcium signaling[1].
Abz-FR-K(Dnp)-P-OH is an angiotensin I-converting enzyme (ACE) substrate and an internally quenched fluorogenic substrate for real time fluorescent assay[1].
Glyoxalase I inhibitor is a potent Glyoxalase I inhibitor, candidate for anticancer agents.
Hydroxocobalamin hydrochloride (Vitamin B12a hydrochloride) is a naturally occurring vitamin B12 form found in food and used as a dietary supplement in the treatment of vitamin B12 deficiency.