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.

BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction (IC50: 21 nM).

JHU37152 (JHU 37152) is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

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.

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.

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

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)

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neuronsin vivo.2It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose. 1.Claffey, M.M., Helal, C.J., Verhoest, P.R., et al.Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitorsJ. Med. Chem.55(21)9055-9068(2012) 2.Lai, B., Li, M., Hu, A., et al.The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learningDev. Neurobiol.78(9)859-872(2018)

Mpro inhibitor N3 hemihydrate is a potent antagonist of the SARS-CoV-2 main protease (Mpro), with an EC50 of 16.77 μM against SARS-CoV-2. It specifically inhibits Mpro in various coronaviruses, including SARS-CoV, MERS-CoV, HCoV-229E (IC50 4.0 μM), FIPV (IC50 8.8 μM), and MHV-A59 (IC50 2.7 μM) [1][2].

Z-Ala-Ala-Asn-AMC, also known as Cbz-Ala-Ala-Asn-AMC, serves as a substrate for legumain. The overexpression of legumain in 293 HEK-Leg cells results in efficient cleavage of Cbz-Ala-Ala-Asn-AMC.

V-9302 hydrochloride is a potent and selective competitive antagonist that inhibits transmembrane glutamine flux by specifically targeting the amino acid transporter ASCT2 (SLC1A5), and not ASCT1. In HEK-293 cells, V-9302 hydrochloride effectively inhibits ASCT2-mediated glutamine uptake with an IC50 value of 9.6 μM.

(S)-BAY-293 is a potent pan-KRAS inhibitor used in the study of primary non-small cell lung and pancreatic cancers.