reporter

Semaglutide is a glucagon-like peptide 1 receptor (GLP-1R) agonist(EC50 of 6.2 pM in a reporter assay using BHK cells expressing the human receptor).

Adavivint (SM04690) is a selective inhibitor of the typical Wnt signaling pathway. In SW480 cells, EC50=19.5 nM was measured using high-throughput TCF LEF reporter gene experiments.

YAP-TEAD-IN-3 is an inhibitor of YAP TAZ-TEAD interactions with an IC50 of 9 nM for Avi-human TEAD (4217-434). YAP-TEAD-IN-3 inhibits YAP reporter gene expression (IC50 = 0.048 μM) and NCI-H2052 cell proliferation (IC50 = 0.048 μM).

LOM612 is a potent and specific FOXO relocator that induces nuclear translocation of the FOXO3a reporter protein as well as endogenous FOXO3a and FOXO1 in a dose-dependent manner in U2OS cells, down-regulates the expression of c-Myc and cyclin D1, and has anti-proliferative effects in human cancer cell lines.

IL-4 inhibitor is an inhibitor of IL-4.1It binds to IL-4 with a Kdvalue of 1.8 μM and inhibits IL-4 activity in a cell-based reporter assay (EC50= 1.81 μM). It is selective for IL-4 over IL-13 (EC50= 18.2 μM). IL-4 inhibitor inhibits IL-4-induced STAT6 phosphorylation in THP-1 monocytes (EC50= 3.1 μM), indicating inhibition of the IL-4-JAK1-STAT6 signaling pathway.

ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50= 1.1 μM in a reporter assay).1It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50= 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated na?ve cord blood human CD4+T cells into Th17 T helper cells.

Ro5-3335 (CBFβ-Runx1 inhibitor II) is core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). Ro5-3335 represses RUNX1 CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. Ro5-3335 also reduces the leukemia burden in a mouse model. Attenuates RUNX1-dependent hematopoiesis in zebrafish embryos. It also is a Tat antagonist and inhibits HIV-1 replication in vitro.

4-Azido-L-phenylalanine hydrochloride (p-Azido-L-phenylalanine hydrochloride) is an unnatural amino acid used as an effective vibrational reporter of local protein environments.

GSK9027 (GR agonist 23a) is a nonsteroidal glucocorticoid receptor (GR) agonist.GSK9027 is a partial agonist on the 2×GRE reporter gene compared to dexamethasone and is less active than dexamethasone activity.

BAR501 impurity is an impurity found in the preparation of BAR501 that acts as an agonist of the G protein-coupled bile acid-activated receptor (GP-BAR1). BAR501 impurity (10 μM) induces a 150% increase in luciferase activity in a GP-BAR1 reporter gene assay

ARS-1323-alkyne is a switch-II pocket (S-IIP) inhibitor and a conformational specific chemical reporter of KRASG12C nucleotide state in living cells.

Atorvastatin ethyl ester, a derivative of Atorvastatin, exhibits potent inhibition of 9-cis-RA-induced Gal4 reporter activity.

Silvestrol aglycone is an analogue of Silvestrol, inhibits protein translation initiation in cancer cells(EC50s of 10 and 200 nM for myc-LUC and tub-LUC luciferase reporter protein translation, respectively), with nti-cancer activity.

TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC50 of 1.9 nM and a reporter gene IC50 of 6.1 nM.

Atorvastatin methyl ester is a derivative of Atorvastatin. It inhibits the 9-cis-RA-induced Gal4 reporter activity more strongly than Atorvastatin.

KY1220 destabilizes both β-catenin and Ras by targeting the Wnt β-catenin pathway. It has an IC50 of 2.1 μM in HEK293 reporter cells.

HPG1860, an agonist of the farnesoid X receptor (FXR), induces luminescence in reporter gene assays utilizing HEK293T cells expressing human FXR, with an EC50 value of 18 nM. In vivo studies demonstrate that HPG1860 (administered at 1, 3, or 10 mg kg daily) reduces serum alanine aminotransferase (ALT) and total cholesterol levels in a mouse model of non-alcoholic steatohepatitis (NASH), which was induced by a high-fat diet and carbon tetrachloride (CCl4). Additionally, this compound decreases hepatic inflammation, fat levels, and fibrosis.

Lipid N2-3L is an ionizable cationic lipid with a pKa of 8.99, utilized in the formation of supramolecular lipid nanoparticles (SMLNPs) for enclosing mRNA in both in vitro and in vivo applications. Lipid N2-3L-containing SMLNPs accumulate at the injection site and draining lymph nodes in mice, featuring a luciferase reporter gene. Additionally, SMLNPs made with Lipid N2-3L that encapsulate ovalbumin mRNA and the Toll-like receptor 7 8 (TLR7 8) agonist R-848 serve as adjuvants. These enhance dendritic cell maturation and antigen presentation, reducing tumor volume and increasing survival rates in MC-38-OVA colon cancer mouse models.

Lipid 29 is an unsaturated, ionizable cationic lipid that facilitates the formation of lipid nanoparticles (LNP) used for intrabody mRNA delivery. When integrated into LNPs encapsulating luciferase reporter gene mRNA, intravenous injection of these LNPs induces bioluminescence in the lungs and spleen of mice.

119-23 is an ionizable cationic lipid frequently utilized in the preparation of lipid nanoparticles (LNPs) for in vivo mRNA delivery. Lipid nanoparticles that include 119-23 and encapsulate mRNA reporter molecules demonstrate a higher transfection efficiency in mouse muscle compared to LNPs containing SM-102 or DLin-MC3-DMA. Additionally, the accumulation of 119-23-containing LNPs in immune cells within the liver and spleen of mice is significantly greater than that of LNPs with SM-102. Furthermore, LNPs containing 119-23 and encoding human erythropoietin (hEPO) mRNA can elevate serum hEPO levels in mice.

PF-03654764 exhibits high affinity for the human H3 receptor, but displays significantly lower affinity for the rat H3 receptor, with over 1000-fold selectivity against other human histamine receptor subtypes (H1, H2, and H4). In functional assays measuring cAMP using reporter gene assays (β-lactamase) conducted in HEK293 cells stably expressing the full-length human or rat H3 receptor, PF-03654764 demonstrated potent antagonist properties.

ZG-2033 (Compound 26) is an orally active HIF-2α agonist that exhibits nanomolar activity (EC50 = 490 nM) in a luciferase reporter assay. It demonstrates an anti-anemic effect and shows synergistic effects with AKB-6548 in anemia, making it useful for the study of renal anemia.

Lipid C2 is an ionizable cationic lipid utilized in the formation of lipid nanoparticles (LNP) for the delivery of mRNA in vivo. LNPs containing Lipid C2 and encapsulating mRNA reporter genes specifically accumulate in the liver and spleen of mice, while avoiding the heart, lungs, and kidneys. Additionally, LNPs with Lipid C2 that encapsulate mRNA encoding Epstein-Barr virus (EBV) protein Latent Membrane Protein 2 (LMP-2), when combined with anti-programmed cell death protein 1 (PD-1) antibodies, have been shown to reduce tumor size, reverse T cell exhaustion, increase the percentage of CD3+CD8+ central T cells and CD3+CD8+ effector memory T cells in the spleen, and decrease the percentage of CD3+T cells expressing Pd-1 in a CT26 mouse model of EBV-infected colon cancer.

CDD-1431 is a highly selective BMPR2 kinase inhibitor with a Kiapp of 20.6 nM. It inhibits BRE reporter gene activity, exhibiting an IC50 of 4.87 μM. BMPs regulate cellular processes across various tissue types such as the kidneys, skeletal muscle, heart, and reproductive organs, and can induce ectopic bone formation.