a-121

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

A-1211212 (BCL2-IN-1) is a potent and selective Bcl-2 inhibitor. It promotes lymphocyte apoptosis, alters colonic mucosa in mice, and improves inflammation.

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

A-1210477-piperazinyl is a compound that specifically targets and binds to the protein myeloid cell leukemia 1 (MCL1) [myeloid cell leukemia 1]. This compound is utilized in PROTAC technology, harnessing the ability to selectively degrade target proteins.

A-1210477 is an effective and specific MCL-1 and Bcl-2 inhibitor (Ki/IC50: 0.454/26.2 nM).

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, with little or no activity against human Nav1.5 or Nav1.7 channels.

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

Bevacizumab, a humanized monoclonal antibody, specifically and with high affinity binds to all isoforms of VEGF-A.

ADTL-SA1215 is a selective SIRT3 activator with SIRT3 deacetylase activity that inhibits the proliferation and migration of human breast cancer MDA-MB-231 cells through the SIRT3-driven autophagy/mitochondrial autophagy signaling pathway, and can be used in the study of triple negative breast cancer.

MDL-104168 is a macrocyclic HIV-protease inhibitor.

Secretin (33-59), rat (TFA) is a 27-aa peptide, which acts on secretin receptor, and enhances the secretion of bicarbonate, enzymes, and K+ from the pancreas[1][2].

Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate p

TP508 TFA is a nonproteolytic thrombin peptide. TP508 TFA activates endothelial NO synthase (eNOS) and stimulates the production of NO in human endothelial cells. It activates endothelial cells and stem cells to revascularize and regenerates tissues.

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.

MB-07729 is a potent non-competitive inhibitor of fructose-1,6-bisphosphate with IC50 values of 189, 121 and 31 nM in rat, monkey and human, respectively, for the study of diabetes.

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.

LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1. LSD1-IN-5 is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM.

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.

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.

5-HT2A receptor agonist-10 (Compound (R)-I-121.HCl) acts as a 5-HT2A receptor agonist with IC50 values of 2192.39 nM for h5-HT2A and 33.57 nM for h5-HT1A. It is applicable in research related to psychiatric disorders, mental illnesses, and central nervous system diseases.

Anxiolytic/nonsedative agent-1 (TCS 1205) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo.

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).