a 293

V-9302 (V9302) is a competitive antagonist of transmembrane glutamine flux that selectively and potently targets the amino acid transporter ASCT2 (IC50: 9.6 uM).

AHR antagonist 4 is a potent aryl hydrocarbon receptor (AHR) antagonist(example 293; IC50: 82.2 nM).It has anti-cancer effects.

B-TPMF is a highly efficient and selective KCa2.1 channel inhibitor with an IC50 of 31 nM, interacting with the serine residue at position 293 to inhibit KCa2.1.

AVE1231 is a TASK-1 channel blocker that inhibits TASK-1 and can be used in the study of atrial fibrillation.

Dooku1 is an analog of Yoda1 and a selective antagonist of endogenous Piezo1 channels. Dooku1 inhibits Ca2+ entry induced by 2μMYoda1 with IC50 values of 1.3μM (in HEK 293 cells) and 1.5μM (in HUVEC). Dooku1 inhibits Yoda1-induced aortic relaxation.

TSHR antagonist S37a is a selective, orally bioavailable TSHR (thyroid-stimulating hormone receptor) antagonist that inhibits TSH-induced cyclic adenosine monophosphate (cAMP) in TSHR-expressing HEK 293 cells, suitable for studying Graves' orbitopathy.

Alniditan is a receptors agonist of 5-HT1B/1D in HEK 293 cells (IC50: 1.7 and 1.3 nM). For 5-HT1B/1D receptors, the pKi values are 8.96 and 9.40, respectively.

GNE-0946 is a potent and selective agonist of RORγ, with an EC50 of 4 nM in HEK-293 cells.

GNE-6468 is a potent and selective agonist of RORγ(RORc) (EC50: 13 nM for HEK-293 cell).

Praliciguat (IW-1973) stimulates sGC in HEK-293 cells (EC50: 197 nM). Praliciguat is an effective and orally active soluble guanylate cyclase stimulator. It also enhances NO signaling and acts as a vasodilator.

NPS-2143 (SB 262470A) is a novel potent and selective antagonist of Ca(2+) receptor.

IBC 293 is selective for GPR109B over niacin receptor GPR109A. IBC 293 is a highly selective agonist for GPR109B, a human orphan G-protein-coupled receptor expressed in adipocytes.

AGH-107 is a highly selective 5-HT7 receptor agonist that can cross the blood-brain barrier, featuring a Ki value of 6 nM and an EC50 value of 19 nM. Demonstrating high selectivity for central nervous system targets, AGH-107 also exhibits high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.

CD73-IN-19 (Compound 4ab) is an inhibitor of CD73, demonstrating a 44% inhibition rate of CD73 enzyme activity at 100 μM. It entirely counters T cell proliferation blockade triggered by TCR activation (induced by CD73 activity) at 10 μM and 100 μM and inhibits hA2A receptor activity in HEK-293 cells with a Ki of 3.31 μM. CD73-IN-19 holds potential for research in the field of immune diseases.

17β-HSD5 inhibitor 1 (Compound 29) is a potent inhibitor of 17β-HSD5, exhibiting an IC50 value of 2.9 nM in HEK-293 cells that overexpress human 17β-HSD5.

JN122 is a spiroindoline-containing molecule that acts as an MDM2 inhibitor. It disrupts the MDM2/p53 protein-protein interaction, exhibiting potent antitumor effects in vivo. JN122 demonstrates antiproliferative activity, with IC50 values of 39.6 nM in HCT-116 cells and 4.28 μM in HEK-293 cells. It induces the activation of p53 and its target genes, halts cell cycle progression, and triggers apoptosis.

Amitifadine hydrochloride (EB-1010 hydrochloride) is a triple reuptake inhibitor (TRI) or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).

Ebsulfur is a benzisothiazolone parasitic inhibitor targeting the trypanothione reductase (TryR) of Trypanosoma brucei, with an IC50 value ranging from 61 to 293 nM for this parasite. Ebsulfur is utilized in the study of African trypanosomiasis.

Bcl-2-IN-20 (Compound 81) is a Bcl-2 inhibitor with an IC50 of less than 10 μM, achieving a 79.1% inhibition rate at 9 μM. It demonstrates cytotoxicity in cell lines such as SK-MEL-28 (IC50 > 10 μM), A549 (IC50 = 6.1 μM), HepG2 (IC50 > 10 μM), MCF-7 (IC50 = 8.9 μM), HCT116 (IC50 > 10 μM), and HEK-293 (IC50 = 14.1 μM). Bcl-2-IN-20 also promotes the generation of ROS, inducing apoptosis and DNA damage.

ARN-6039, an orally available inverse agonist of RORγ, targets Autoimmune Neuroinflammatory Demyelinating Disease. Its efficacy was demonstrated in a RORγ-activated IL-17A Prom/LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 release from CD4+T cell assays (220 nM).

AMP-579 is an adenosine A1 receptor agonist. AMP-579 also acts as a A2b-adenosine receptor agonist in human 293 cells and rabbit hearts.

GNE-293 is a potent and selective PI3Kδ inhibitor.

PIK-293 is a PI3K inhibitor, for PI3Kδ( IC50=0.24 μM), and less potent for PI3Kα/β/ γ.

PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50= 31 nM).1It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer's disease.4 1.March, D.R., Proctor, L.M., Stoermer, M.J., et al.Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activityMol. Pharmacol.65(4)868-879(2004) 2.Jain, U., Woodruff, T.M., and Stadnyk, A.W.The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10Br. J. Pharmacol.168(2)488-501(2013) 3.Staab, E.B., Sanderson, S.D., Wells, S.M., et al.Treatment with the C5a receptor/CD88 antagonist PMX205 reduces inflammation in a murine model of allergic asthmaInt. Immunopharmacol.21(2)293-300(2014) 4.Fonseca, M.I., Ager, R.R., Chu, S.-H., et al.Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's diseaseJ. Immunol.183(2)1375-1383(2009)