Methyl caffeate, an antimicrobial agent, shows moderate antimicrobial and prominent antimycobacterial activities. Methyl caffeate also exhibits α-glucosidase inhibition activity, oxidative stress inhibiting activity, anti-platelet activity, antiproliferative activity in cervix adenocarcinoma and anticancer activity in lung and leukmia cell lines[1].
7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
Metrifonate is an irreversible organophosphate acetylcholinesterase inhibitor that is used as an insecticide for the control of flies and roaches.
Fast red TR salt hemi (zinc chloride) is a diazonium dye with red color[1].
Boc-NH-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
KDM4-IN-4 (compound 47) is a potent histone lysine demethylase 4 (KDM4) inhibitor with a modest affinity binding to ~80 μM for KDM4A-Tudor domain. KDM4-IN-4 can inhibit H3K4Me3 binding to the Tudor domain in cells with an EC50 value of 105 μM. KDM4-IN-4 can be used for researching anticancer[1].
LY-368975 is a potent and selective inhibitor of the norepinephrine (NE) reuptake site. LY-368975 reduces food consumption in rodents.
Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside (compound 1) is a lignan with anti-HBC activity. Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside targets HBV surface antigen with IC50s of 0.58 mM (HBsAg) and >2.4 mM (HBeAg). Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside can be isolated from star anise[1].
BRL 52537 hydrochloride is a highly selective κ-Opioid receptor (KOR) agonist with Kis of 0.24 nM and 1560 nM for κ and μ subtypes, respectively. BRL 52537 hydrochloride decreases ischemia-evoked NO production as a potential mechanism of neuroprotection. BRL 52537 hydrochloride attenuates early stroke damage[1].
FR-167653 is a selective p38 MAPK inhibitor.
Niflumic acid-13C6 is the 13C6 labeled Niflumic acid. Niflumic acid, a Ca2+-activated Cl- channel blocker, is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.
Benzoylaconine(Isaconitine; Pikraconitin) is an alkaloid in the Chinese traditional medicine Radix Aconiti Lateralis Preparata (Fuzi).
Chalcone dibromide is a useful synthon in the synthesis of a large number of bioactive molecules such as pyrazolines, hydroxy pyrazolines, isoxazoles etc. Chalcone dibromide possesses antioxidant effects against tumor cells by inhibiting superoxide production and lipid peroxidation. Chalcone dibromide can be used for cancer disease research[1].
eIF4A3-IN-7 is a potent inhibitor of eIF4A3. eIF4A3-IN-7 has the potential for researching cancer and other dysproliferative diseases (extracted from patent WO2019161345A1, Compound 8)[1].
CrBKA is a fluorogenic small-molecule substrate of SIRT6 with weak activity[1].
NBQX is a highly selective and competitive AMPA receptor antagonist.
(R,S,R)-ML334 is the inactive isomer of ML334 (HY-110258), and can be used as an experimental control. ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity[1][2].
MC-Val-Cit-PAB-indibulin has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-indibulin is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
CCG-203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gαo protein-protein interaction in vitro with an IC50 of 17 nM.
TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1[1].
Biotin-C4-amide-C5-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
RSV L-protein-IN-5 (compound E) is a potent inhibitor of Respiratory syncytial virus (RSV) (EC50=0.1 μM). RSV L-protein-IN-5 inhibits Polymerase (IC50=0.66 μM),and blocks RSV mRNA synthesis by inhibiting guanylation of viral transcripts. RSV L-protein-IN-5 shows moderate cytotoxicity (CC50=10.7 μM,HEp-2),also exhibits activity and lowers virus titers in mouse models of RSV infection[1].
Palonidipine is a calcium antagonist which is potential for the therapy of angina-pectoris and hypertension[1][2][3].
Bemoradan (compound 10a) is an orally active and selective canine Phosphodiesterase (PDE) fraction III inhibitor. Bemoradan is a long-acting, potent, inotropic vasodilator and a novel cardiotonic agent, and can be used in congestive heart failure research[1].
BAY-850 is a potent and isoform selective ATPase family AAA domain-containing protein 2 (ATAD2) inhibitor, with an IC50 of 166 nM.
Elarekibep (PRS-060) (AZD1402) is a high affinity, slowly dissociating, long-acting full antagonist of IL-4Ra. Elarekibep can be used for the research of T2 endotype asthma[1].
Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively.
Zymostenol (5a-Cholest-8-en-3b-ol) is a late-stage precursor in the biosynthesis of cholesterol. Zymostenol is a RORγ agonist (EC50: 1 μM)[1][2][3].
6-Azido-D-lysine hydrochloride is a click chemistry reagent containing an azide[1].
β-Lapachone is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.