Dihydroaltenuene B is a potent mushroom tyrosinase inhibitor with an IC50 of 38.33 µM. Dihydroaltenuene B shows the hydrogen bonding interactions between the 3-OH and 4’-OH and the His244, Met280 and Gly281 residues of tyrosinase[1].
Lycopsamine N-oxide, an N-oxide of Lycopsamine which is a pyrrolizidine alkaloid, can be found in honey and bee pollen[1].
(d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin (SKF 100273) is a vasopressin V1 receptor selective antagonist[1].
TSR-033 is a high affinity human IgG4 antibody targeting LAG-3 (lymphocyte activation gene-3), a co-receptor associated with impaired T cell function and often co-expressed with PD-1, that enhances T cell function and PD-1 blocking activity in vitro and in vivo. TSR-033 has anti-tumor activity[1].
Loperamide (ADL 2-1294) is a selective μ opioid receptor agonist with Kis of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide can be used as an antidiarrheal agent[1].
Hoechst 33258 trihydrochloride is a fluorescent dyes, which can be used as a cell dye for DNA.
Fmoc-β-HoArg(Pbf)-OH is an arginine derivative[1].
7-Methylguanosine is a novel cNIIIB nucleotidase inhibitor with IC50 value of 87.8 ± 7.5 µM.
Nα-Fmoc-N(im)-trityl-L-histidine pentafluorophenyl ester is a histidine derivative[1].
H-Thr(Me)-OH is a threonine derivative[1].
Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine.IC50:Target: 5-hydroxytryptamine1B/1D (5-HT1B/1D) ReceptorAlmotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. Almotriptan showed low nanomolar affinity for the 5-HT(1B) and 5-HT(1D) receptors in several species, including the human, while affinity for 5-HT receptors other than 5-HT(1B/1D) was clearly less. Almotriptan did not exhibit significant affinity for several non-5-HT receptors studied up to 100 microM. Almotriptan inhibited forskolin-stimulated cyclic AMP accumulation in HeLa cells transfected with 5-HT(1B) or 5-HT(1D) human receptors [1]. Almotriptan had a mild antiemetic effect and a slight, transient diuretic effect in dogs, although the latter effect is probably of no clinical relevance. In addition, no effect on the respiratory system of conscious guinea pigs was observed following almotriptan treatment. These results indicate that almotriptan has a favourable safety profile with respect to the central nervous, renal and respiratory systems [2].
c-Met-IN-10 (compound 26a) is a highly potent c-Met kinase inhibitor with an IC50 value of 16 nM. c-Met-IN-10 has inhibitory activity against cancer cells A549, H460 and HT-29 with IC50s of 0.56 ~ 1.59 μM. c-Met-IN-10 suppresses the colony formation on HT-29 cells, induces HT-29 and A549 cells apoptosis, and inhibits A549 cells motility. c-Met-IN-10 can be used for researching anticancer[1].
DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinaseinhibitor with IC50/EC50 of 105 nM/87 nM; 4-fold less potent for DDR2 (IC50= 413 nM).IC50 value: 105 nM [1]Target: DDR1We confirmed the observed binding to DDR1 using an enzymatic kinase assay employing the Lanthascreen technology. In this assay DDR1-IN-1 exhibits an IC50 of 105 nM against DDR1 and 413 nM against DDR2. DDR1-IN-1 and DDR1-IN-2 inhibited basal DDR1 autophosphorylation with an EC50 of 86 nM and 9 nM, respectively. Both DDR1-IN-1 and DDR1-IN-2 demonstrated weaker inhibition of DDR1 autophosphorylation in the absence of collagen stimulation.
Brombuterol D9 hydrochloride (Bromobuterol D9 hydrochloride) is a deuterium labeled Brombuterol hydrochloride. Brombuterol hydrochloride is a β-adrenergic receptor agonist[1].
Cutamesine dihydrochloride (SA4503 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.
FN-439 is a selective collagenase-1 inhibitor. FN-439 inhibits collagenase-1 with an IC50 value of 1 μM. FN-439 can be used for the research of cancer and inflammation[1][2].
Soluflazine is a nucleoside transport inhibitor with anticonvulsant action. Soluflazine can be used as an antiepileptic agent[1].
Bromo-PEG2-C2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
EGLU ((2S)-α-Ethylglutamic acid; (2S)-α-EGLU) is a potent and competitive mGluR-2 receptor antagonist. EGLU interacts with (lS,3S)-ACPD-sensitive site with a Kd value of 66 μM. EGLU is an antidepressant agent[1].
Naxagolide hydrochloride is an agonist of D2. Naxagolide hydrochloride can be used in study Parkinsonism[1].
Osalmid is a ribonucleotide reductase small subunit M2 (RRM2) targeting compound; suppresses ribonucleotide reductase activity with an IC50 of 8.23 μM.
AM6701 is a potent FAAH/MAGL inhibitor (equipotent inhibitory IC50: 1.2 nM) with neuroprotective effects[1].
SF1126 is a clinically relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis[1].
Glycine cresol red is a complexometric indicator. Glycine cresol red forms coloured complexes with Al3+, Ga3+ and In3+ ions in aqueous solutions. Glycine cresol red can been used for the spectrophotometric determination of inorganic ions. Glycine cresol red can be used as a stain in neurohistology[1][2].
15-Methoxymkapwanin is a neo-clerodane diterpene compound isolated the leaf surface exudate of Dodonaea angustifolia[1].
Mefenamic Acid-d3 is the deuterium labeled Mefenamic acid. Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
Gymnemagenin is a triterpenoid isolated from G. sylvestre. Gymnemagenin is an agent for diabetes and obesity and also possesses antiviral properties[1][2].
Des(benzylpyridyl) Atazanavir is a metabolite of Atazanavir, which is a HIV protease inhibitor. Des(benzylpyridyl) Atazanavir can be used for the research of HIV-1 infection[1].
S-(2-Carboxyethyl)-L-cysteine (S-Carboxyethylcysteine) is a non-protein (modified) sulfur amino acid. S-(2-Carboxyethyl)-L-cysteine is present in Acacia seed. S-(2-Carboxyethyl)-L-cysteine can affect the seed’s protein use in rats. S-(2-Carboxyethyl)-L-cysteine suppresses the methionine-induced growth rate, and has a negative effect on the plasma amino acid levels in rats[1].
Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.