hek 293 cells

OS-3-106 is a novel arylamide phenylpiperazines, as partial agonists at the D3R in the adenylyl cyclase inhibition assay.

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).

DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115 200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.

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.

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.

4 -C18 EGCG is an effective inhibitor of α-amylase and α-glucosidase, with IC50 values of 3.74 μM and 0.81 μM respectively. It inhibits carbohydrate-hydrolyzing enzymes, reducing oxidative stress and inflammation, and demonstrates anti-diabetic activity. Additionally, 4 -C18 EGCG downregulates pro-inflammatory cytokines and exhibits cytotoxicity at 50 μM in primary human peripheral blood mononuclear cells (PBMC), and non-cancerous cell lines 3T3-L1 and HEK 293.

4''-C18 EGCG is an effective inhibitor of α-amylase and α-glucosidase, with IC50 values of 3.74 and 0.81 μM, respectively. This compound suppresses carbohydrate-hydrolyzing enzymes, reduces oxidative stress and inflammation, and exhibits anti-diabetic activity. Moreover, 4''-C18 EGCG downregulates pro-inflammatory cytokines and demonstrates cytotoxicity at 50 μM against primary human peripheral blood mononuclear cells (PBMC), as well as non-cancerous cell lines 3T3-L1 and HEK 293.

Gamma-Glu-AbuTFA is the TFA salt form of Gamma-Glu-Abu. This compound acts as an agonist for the calcium sensing receptor (CaSR), activating CaSR in HEK-293 cells with an EC50 of 0.21 μM.

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.

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).

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.

KPC-2-IN-1, a boronic acid derivative, serves as an effective KPC-2 inhibitor with a K i of 0.032 μM, augmenting cefotaxime's efficacy against KPC-2 expressing E. coli. It demonstrates good tolerance in human HEK-293 cells, rendering it valuable for researching E. coli's resistance to β-lactam antibiotics [1] [2].

Apelin-36(human) TFA, an endogenous agonist of the orphan G protein-coupled receptor APJ, exhibits a potent EC50 of 20 nM and high affinity (pIC5 50 = 8.61) for human APJ receptors in HEK 293 cells. It is involved in significant cardiovascular and metabolic activities. Furthermore, Apelin-36(human) TFA can inhibit the entry of certain HIV-1 and HIV-2 strains into NP2 CD4 cells expressing the APJ receptor. [1] [2] [3] [4]

Apelin-17(human, bovine) TFA is an endogenous agonist of the orphan G protein-coupled receptor APJ, demonstrating affinity for human APJ receptors on HEK 293 cells with a pIC50 value of 9.02. It also blocks the entry of certain HIV-1 and HIV-2 strains into NP2 CD4 cells that express the APJ receptor [1] [2] [3].

AC1903 is a specific inhibitor of TRPC5 channel, and has been shown to suppress severe proteinuria and prevent podocyte loss.

SB 206553 is a 5-HT2C inverse agonist that can attenuate methamphetamine-seeking behavior in rats. It exhibits activity for 5-HT2 receptor ligands with pKi values of 5.6 nM (5-HT2A), 7.7 nM (5-HT2B), and 7.8 nM (5-HT2C) in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors. SB 206553 can be used for research into psychostimulant abuse disorders [1].

hVEGF-IN-3 (compound 9) serves as an effective inhibitor of hVEGF. It inhibits the proliferation of HT-29, MCF-7, and HEK-293 cells with IC50 values of 61, 142, and 114 μM, respectively.

JHU37160 (JHU 37160) is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.

Endogenous APJ receptor agonist (EC50 = 20 nM) that is secreted by adipocytes. Binds with high affinity to human APJ receptors expressed in HEK 293 cells (pIC50= 8.61). Involved in regulation of cardiovascular function, fluid homeostasis and feeding. Bloc