AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects[1][2].
BRD4-IN-3 (compound 141) is a potent BRD4 inhibitor with an IC50 of <0.5 µM. BRD4-IN-3 shows cytoxicity for MYC-Raji with an IC50 value of >1 µM[1].
Danirixin is a selective, and reversible CXCR2 antagonist, with IC50 of 12.5 nM for CXCL8.
XL413 hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.
Dodoviscin I is an adipogenesis agent that increases triglyceride content in 3T3L1 mouse fibroblasts[1].
N-(4-Anilino-1-naphthyl)maleimide is a fluorescent probe that can be used to detect thiol groups in proteins. N-(4-Anilino-1-naphthyl)maleimide reacts with thiol groups and immediately produces a stable fluorescent compound with the λex=355 nm, λem=448 nm[1].
Bismuth subcitrate potassium is an antibiotic against 12 C. pyloridis strains with MIC50 of 8 ug/ml[1]. Bismuth subcitrate potassium is used to treat diseases of the upper gastrointestinal tract infected with Helicobacter pylori[2].
5’-O-DMTr-2’-OMeU-methyl phosphonamidite is a purine nucleoside analog. 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].
Losatuxizumab (ABT-806) is an anti-EGFR monoclonal antibody. Losatuxizumab binds to EGFR with EC50s of 0.96 nM for EGFR wild-type, 0.09 nM for EGFRC271A,C283A, 0.12 nM for EGFRvIII, 0.66 nM for EGFR1-501. Losatuxizumab can be used for research of EGFR-expressing cancers[1][2].
Teneligliptin hydrobromide hydrate is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM[1].
Monomethyl auristatin E (MMAE) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
Monomethyl auristatin E intermediate-16 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs)[1].
Cefaclor monohydrate is an effective antibiotic agent, and specifically binds to penicillin-binding protein 3 (PBP 3)[1].
AMG 333 is a potent and highly selective TRPM8 antagonist with an IC50 of 13 nM.
Piperazine Dihydrochloride-d8 is the deuterium labeled Piperazine Dihydrochloride[1].
Gidazepam is an agonist of GABA receptor channels (GABA RCs).
PGS-IN-1 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase with an IC50 of 1.05 μM.
RR-11a is a synthetic enzyme inhibitor of Legumain.
Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels.
APC-6860 is a trypsin-like serine proteases inhibitor with ki values of 0.21 and 0.44 μM for uPA and trypsin, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has ki values of 0.1 and 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer[1][2].
Sodium carboxymethyl cellulose is the sodium salt of cellulose arboxymethyl and frequently used as viscous agent, paste and barrier agent.
HBV-IN-8 is a potent HBV inhibitor with an EC50 of 287.9 nM (WO2021213445A1, compound 13)[1].
QX-314 bromide is a membrane-impermeable permanently charged sodium channel blocker[1].
3,4-Dicaffeoylquinic acid is a reference substance of a common phytochemical found in Echinacea (Echinacea sp.); dietary supplement, herb, or plant testing applications with this reference material include material characterization, adulterant identification, or method validation.
Pibrentasvir is a novel and pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with EC50s ranging from 1.4 to 5.0 pM against HCV replicons containing NS5A from genotypes 1 to 6.
UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2, a pyrimidine salvage enzyme) with an IC50 value of 16.6 μM. UCK2 can replace dihydroorotate dehydrogenase (DHODH), in a certain extent, in infected or rapidly dividing cells to continue efficient uridine salvage. UCK2 Inhibitor-3 also inhibits DNA polymerase eta and kappa with IC50s of 56 μM and 16 μM[1].
Epimedokoreanin B is a natural flavonoid with anticancer, anti-inflammatory and antibacterial effects. Epimedokoreanin B inhibits the growth of lung cancer cells through endoplasmic reticulum stress-mediated Apoptosis accompanied by autophagosome accumulation. Epimedokoreanin B is an anti-periodontitis agent that inhibits gingipains and Porphyromonas gingivalis growth and biofilm formation[1][2][3].
Amodiaquine dihydrochloride dihydrate is a histamine N-methyltransferase inhibitor, used as an antimalarial and anti-inflammatory agent.Target: histamine N-methyltransferaseAmodiaquine has been shown to be more effective than chloroquine in treating chloroquine-resistant Plasmodium falciparum malaria infections and may afford more protection than chloroquine when used as weekly prophylaxis. Amodiaquine is generally well tolerated.