hek293 reporter cells

KY1220 通过靶向 Wnt β-连环蛋白通路，使 β-连环蛋白和 Ras 不稳定。 它在 HEK293 报告细胞中的 IC50 为 2.1 μM。

PF-03654764对人类H3受体具有高亲和力，并对大鼠H3受体具有较低亲和力，同时对其他人类组胺受体亚型（H1，H2和H4）具有超过1000倍的选择性。在使用报告基因测定法（β-内酰胺酶）并在稳定表达全长人类或大鼠H3受体的HEK293细胞中测量cAMP的功能性实验中，PF-03654764展示了强大的拮抗剂特性。

YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid accumulation in mice fed a high-fat diet, but not mice fed normal chow, when administered at a dose of 40 mg/kg every other day for 11 weeks.References1. Obianom, O.N., Ai, Y., Li, Y., et al. Triazole-based inhibitors of the Wnt/β-catenin signaling pathway improve glucose and lipid metabolism in diet-induced obese mice. J. Med. Chem. 62(2), 727-741 (2019). YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid accumulation in mice fed a high-fat diet, but not mice fed normal chow, when administered at a dose of 40 mg/kg every other day for 11 weeks. References1. Obianom, O.N., Ai, Y., Li, Y., et al. Triazole-based inhibitors of the Wnt/β-catenin signaling pathway improve glucose and lipid metabolism in diet-induced obese mice. J. Med. Chem. 62(2), 727-741 (2019).

The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors). In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively. KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 is highly cytotoxic at similar concentrations in these cells. KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.

EP4 antagonist 14是一种前列腺素E2（PGE2）受体亚型EP4的拮抗剂，其在使用表达人源受体的HEK293细胞的报告基因测定中的IC50值为1.1 nM。它还能抑制PGE2诱导的同种细胞中的β-阿雷斯汀招募（IC50 = 0.9 nM）。EP4 antagonist 14（10 µM）能减少RAW 264.7巨噬细胞中PGE2诱导的mRNA表达，这些mRNA编码Il-4、巨噬细胞甘露糖受体1（Mrc1）、几丁质酶样蛋白3（Chil3）、趋化因子（C-X-C）基序配体1（Cxcl1）、表达在髓样细胞上的触发受体2（Trem2）和精氨酸酶-1（Arg1）。在体内，EP4 antagonist 14（每天30 mg/kg），结合抗PD-1抗体，能够在CT26小鼠结肠癌模型中抑制肿瘤生长并增加CD8+ T细胞对肿瘤的浸润。