at 121

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

AT-121 hydrochloride is a dual agonist of nociception and mu opioid receptor with Ki values of 3.67 and 16.49 nM, respectively.AT-121 hydrochloride is a safe, non-addictive, pain relieving compound with anti-injury and analgesic activity. AT-121 hydrochloride is a safe, non-addictive, pain relieving compound with anti-injury and analgesic activity.

CMS-121, a quinolone derivative, is an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor. CMS-121 protects HT22 cells against ischemia and oxidative damage (EC50: 7 nM and 200 nM). CMS-121 shows strong neuroprotective, antioxidative, anti-inflammatory, and renoprotective activities.

SKA-121 is a selective KCa3.1 activator (EC50s: 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively).

Antifungal Agent 121 (compound TM11) is a fungicide characterized chemically as a benzimidazole-acrylonitrile derivative.

SMS 121 is a novel CD36 inhibitor that impairs fatty acid uptake and cell viability in acute myeloid leukaemia (AML) cells.

ELQ-121 is a potent inhibitor of the ubiquinol oxidation (QO) site in parasites. It exhibits an in vitro IC50 of 0.05 nM against both chloroquine-sensitive and multi-drug resistant Plasmodium falciparum. ELQ-121 also inhibits Toxoplasma gondii and Neospora caninum with an in vitro IC50 of less than 1 nM. It hinders the proliferation of Bacteroides fragilis tachyzoites with an IC50 of 0.49 nM and induces mitochondrial disruption. Furthermore, ELQ-121 can be formulated into a polyethylene glycol carbonate prodrug, which shows efficacy against P. yoelii in mice. ELQ-121 is applicable for antimalarial research.

YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50=3.4 μM) and 5-lipoxygenase (5-LOX; IC50=6.5 μM). YS121 dose-dependently reduces the production of PGE2 with EC50=12 μM in IL-1β-stimulated A549 cells [1].

GSK121 is an inhibitor of selective PAD4.

PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).

A 121 is a non-polyene antifungal antibiotic. It is active against a number of filamentous fungi including some plant and human pathogens.

Sul-121 has anti-oxidative capacity. In experimental chronic obstructive pulmonary disease (COPD) models, Sul-121 HCl inhibits airway inflammation and hyperresponsiveness (AHR) prospectively through inhibition of oxidative stress.

TX2-121-1 targets HER3 for proteasome-mediated degradation to inhibit HER3-dependent signalling and growth.

RC 121 is a highly potent somatostatin (SRIF) analog.

KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.1 1.Ikeda, H.O., Sasaoka, N., Koike, M., et al.Novel VCP modulators mitigate major pathologies of rd10, a mouse model of retinitis pigmentosaSci. Rep.45970(2014) 2.Kinoshita, H., Maki, T., Yasuda, K., et al.KUS121, a valosin-containing protein modulator, attenuates ischemic stroke via preventing ATP depletionSci. Rep.9(1)11519(2019)

NS2 (114-121), Influenza, is a fragment derived from the nonstructural protein 2 (NS2) of the influenza virus, serving as an epitope for influenza research and useful for studying CD8+ cytotoxic T lymphocyte (CTL) responses in antiviral immunity.

CM121 is a reversible inhibitor of ALDH1A2 that acts specifically on the active site, exhibiting an IC50 of 0.54 μM and a Kd of 1.1 μM. It exerts its inhibitory effect through multiple hydrophobic interactions.

BCI-121 is a substrate-competitive SMYD3 inhibitor that inhibits the proliferation of the cancer cell.

Antibacterial agent 121 (Compound 10) exhibits antibacterial properties against mycobacterial strains and possesses anti-inflammatory activity, making it a promising candidate for Tuberculosis (TB) research [1].

CYP121A1-IN-1 is a potent inhibitor of CYP121A1, demonstrating favorable activity against Mycobacterium tuberculosis (H37Rv MIC 90 ~6.25 μM, ~2.2 μg/mL). It significantly reduces mycocyclosin production by blocking the CYP121A1-mediated conversion of cyclo(l-tyrosyl-l-tyrosyl) to mycocyclosin [1].

Reversin 121, a P-glycoprotein inhibitor, enhances MDR1's ATPase activity and counteracts P-glycoprotein-mediated multidrug resistance, making it useful in cancer research.

Anticancer agent 121, a human lactate dehydrogenase A (hLDHA) inhibitor, exhibits potent anticancer activities, suitable for use in anticancer research [1].

EGFR-IN-121 (compound 15) acts as a dual inhibitor for EGFR and VEGFR-2, with IC50 values of 84 nM and 3.5 nM, respectively.

TAS-121 is an orally active, selective, covalent third-generation mutant EGFR tyrosine kinase inhibitor (EGFR-TKI). It effectively inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM), and Ex19del/T790M mutation (IC50=1.1 nM), as well as wild-type EGFR (IC50=8.2 nM). TAS-121 also inhibits HER2 and HER4 with an IC50 of 110 nM and 2.6 nM, respectively. This compound prevents cellular proliferation by inhibiting the phosphorylation of EGFR and its downstream signaling targets, thereby inducing apoptosis. Additionally, TAS-121 demonstrates antitumor activity in xenograft models such as SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M).