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PNU-74654

CAS No. : 113906-27-7

MCE 站：PNU-74654

产品活性：PNU-74654是Wnt/β-catenin通路的的抑制剂，在NCI-H295 细胞中的IC₅₀值为129.8 μM。

研究领域：Stem Cell/Wnt  |  Apoptosis

作用靶点：Wnt  |  β-catenin  |  Apoptosis

In Vitro: PNU-74654 binds to β-catenin with a K_D of 450 nM. The Tcf3/Tcf4-binding surface on β-catenin contains a well-defined hot spot around residues K435 and R469. The binding mode of PNU-74654 involves the two narrow pockets on either side of this hot spot. In NCI-H295 cells,PNU-74654 significantly decreases cell proliferation 96 h after treatment, increases early and late apoptosis, decreases nuclear beta-catenin accumulation, impairs CTNNB1/beta-catenin expression and increases beta-catenin target genes 48 h after treatment. No effects are observed on HeLa cells. In NCI-H295 cells, PNU-74654 decreases cortisol, testosterone and androstenedione secretion 24 and 48 h after treatment. The SF1 and CYP21A2 mRNA expression as well as the protein levels of STAR and aldosterone synthase are decreased in NCI-H295 cells after 48 h PNU-74654 treatment. In Y1 cells, PNU-74654 impairs corticosterone secretion 24 h after treatment but does not decrease cell viability.

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