reporter

SR11237 is a Pan retinoid X receptor (RXR) agonist. SR11237 causes RXR/RXR homodimers to form and transactivate a reporter gene containing a RXR-response element.

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.

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.

Cudarolimab (IBI101) is a human monoclonal antibody and an OX40 (CD134/TNFRSF4) agonist. Cudarolimab activates the OX40 signaling pathway, promoting the proliferation and activation of effector T cells and enhancing T cell-mediated antitumor immune responses, thereby inhibiting tumor growth. Cudarolimab is indicated for use in solid tumor research.

Semaglutide is a long-acting, selective, competitive GLP-1R agonist and a long-acting analog of human glucagon-like peptide-1, exhibiting potent hypoglycemic, weight-loss, cardioprotective, and neuroprotective effects. Upon activation of the GLP-1R, semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, while also enhancing autophagy and suppressing oxidative stress and apoptosis. Semaglutide also plays a role in regulating mitochondrial function and lipid metabolism. Semaglutide is being investigated for use in type 2 diabetes, obesity, Parkinson’s disease, metabolic and fatty liver diseases (MASLD), and other neurodegenerative and liver diseases, as well as in cancer research.

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 (IAG933) belongs to small molecule inhibitors and is a TEAD-targeted YAP/TAZ-TEAD protein-protein interaction inhibitor (IC50 = 9 nM) with oral activity and selective inhibitory capability against all four TEAD isoforms. This compound is used in antitumor and pro-apoptosis research.

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.

OPN-9652 is a potent and orally active covalent TEAD inhibitor, with a half-maximal inhibitory concentration (IC50) of 0.005 µM against TEAD in MSTO-211H cells, and it targets the central palmitate-binding pocket of TEAD. OPN-9652 can significantly reduce the activity of TEAD-dependent reporter genes and downregulate the expression levels of TEAD target genes (CTGF and CYR61). Notably, OPN-9652 can reverse the resistance of SOX10 knockout (SOX10 KO) resistant cells to the combination of BRAF inhibitor (BRAFi) and MAPK inhibitor (MAPKi), restoring their sensitivity to the drugs. In the xenograft mouse model of BRAF-mutant A375 cells, OPN-9652 can effectively delay the development of tumor drug resistance; specifically, this effect is manifested by a significant delay in the onset of tumor drug resistance after the combination of BRAFi and MEK inhibitor (MEKi) starting from the minimal residual disease (MRD) stage. At present, OPN-9652 can be used as a research tool for scientific research related to melanoma.

SR 1903 is an inverse agonist of RORγ and PPARγ (IC₅₀ = 100 nM and 209 nM, respectively) and an agonist of LXR (EC₅₀ = 154 nM). It exerts anti-inflammatory and anti-diabetic effects in mouse models of collagen-induced arthritis and diet-induced obesity.

ML241 is a potent and selective inhibitors of p97 ATPase.ML241 inhibits degradation of a p97-dependent but not a p97-independent proteasome substrate in a dual-reporter cell line. ML241 may be a novel agent for the chemotherapy of cancer, and provide a rationale for developing pathway-specific p97 inhibitors.

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.

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

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.

HPG1860 is a farnesol X receptor (FXR) agonist that effectively activates FXR-mediated transcriptional activity, with an EC50 value of 18 nM. In vivo studies have shown that HPG1860, administered at doses of 1, 3 or 10 mg/kg daily, reduces serum alanine aminotransferase (ALT) and total cholesterol levels in mouse models of non-alcoholic steatohepatitis (NASH) induced by a high-fat diet and carbon tetrachloride (CCl₄). HPG1860 also reduces levels of liver inflammation, lipid accumulation and fibrosis. Consequently, HPG1860 is suitable for research into metabolic diseases, liver fibrosis, bile acid signalling and FXR-mediated transcriptional regulation.

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.