hek 293 cells

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

KN-62 is a potent and specific Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor with Ki of 0.9 μM.

AC1-IN-1 is a selective inhibitor of adenylyl cyclase type 1 (AC1, IC50 = 0.54 µM).

HG-10-102-01 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2, IC50 of 20.3 nM).

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.

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.

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.

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.

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 competitive transmembrane glutamine flux antagonist that selectively targets the amino acid transporter ASCT2/SLC1A5. V-9302 hydrochloride impedes glutamine uptake mediated by ASCT2 (IC50=9.6 μM), inhibits the mTOR signalling pathway, increases oxidative stress and ROS levels, induces autophagy, and exerts antitumour effects.

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.