β-catenin-in-2

β-catenin-IN-2 是有效的β-catenin 抑制剂。β-catenin-IN-2在结直肠癌中有研究的价值。

PTK7 β-catenin-IN-2（compound 04967）作为PTK7 β-catenin抑制剂，能够阻断PTK7与β-catenin的结合（IC50: 5.6 μM），进而阻断Wnt β-catenin通路的信号传递。此化合物针对依赖Wnt信号通路的细胞生长显示出抑制作用，并具有潜在的抗癌特性。此外，PTK7 β-catenin-IN-2对p53与MDM2的结合亦表现出一定的抑制效力，其IC50值为157.1 μM。

Wnt β-catenin-IN-2 (Compound 3235-0367) 作为Wnt β-catenin信号通路的抑制剂，其IC50和KD值分别为7.1 μM和2.5 μM。该化合物主要用于癌症研究领域。

CHIR-99021 HCl (Laduviglusib HCl) 是GSK-3α β的高效选择性抑制剂，IC50值分别为10 nM和6.7 nM。它对GSK-3表现出显著的选择性，对CDC2、ERK2和其他蛋白激酶的选择性超过500倍。此外，CHIR-99021 HCl 是Wnt β-catenin信号通路的强大激活剂。此外，它在小鼠和人类胚胎干细胞中都表现出增强自我更新的能力。此外，拉杜维格西单盐酸盐诱导自噬[1][2][3]。

TNIK-IN-2 是有效的TNIK 抑制剂，IC50为 1.3337 μM。

Bisdemethoxycurcumin (Curcumin III) 是一种具有抗炎及抗氧化作用的姜黄素。

TNKS-2-IN-1 是一种 TNKS-2 抑制剂。TNKS-2-IN-1 对 TNKS-1 和 TNKS-2有抑制作用，IC50 分别为 259 nM 和 1100 nM。TNKS-2-IN-1 具有抗菌活性，对大肠杆菌和金黄色葡萄球菌具有抑制作用。TNKS-2-IN-1 抑制 NLRP3 炎症小体 （IC505μM）通过抑制ATP刺激的J1A.774细胞释放IL-1β。

FMF-04-159-2是一种高效的共价型细胞周期蛋白依赖性激酶14（CDK14）抑制剂，对CDK14和CDK2的IC₅₀分别为39.6 nM和256 nM。FMF-04-159-2能够减少α-突触核蛋白（α-Syn）在神经元中的聚集并在帕金森病模型中发挥作用，也能够通过减弱Wnt β-catenin信号抑制三阴性乳腺癌（TNBC）的进展和转移。

Tankyrase-IN-2 is a selective, potent and orally active inhibitor of tankyrase with IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively

LZZ-02通过稳定axin 2并减少包括c-Myc和cyclin D1在内的下游蛋白水平，降解β-catenin的表达，从而抑制β-catenin的转录活性，有效缩小源自结肠细胞系的肿瘤异种移植物。

GSK-3β inhibitor24 (Compound 41) 是一种高效的GSK-3β抑制剂，IC50值为0.22 nM。该化合物能够剂量依赖性地增加GSK-3β在Ser9位点的磷酸化，并通过降低p-tau-Ser396的水平来抑制tau蛋白的过度磷酸化。此外，GSK-3β inhibitor24 可上调β-catenin以及神经发生相关标记物(GAP43和MAP-2)，显现出显著的抗阿尔茨海默病(AD)效力。

Cardionogen-2 是一种双相的心脏生成调节剂，根据干预的阶段不同，能够促进或阻碍心脏的形成。它在小鼠胚胎干细胞和斑马鱼胚胎中抑制 Wnt β-catenin 依赖性转录。

TCF4 β-catenin-IN-1 (Compound 8b) 是一种 TCF4 β-catenin 的抑制剂，能够诱导细胞凋亡（apoptosis）。它可以上调 p53、caspase-3、caspase-8、caspase-9 的水平，以及 Bax 蛋白的表达，同时下调 Bcl-2 蛋白的表达。此外，TCF4 β-catenin-IN-1 能抑制 CYP3A4、CYP1A2、CYP2C19，并在癌细胞中展现出优良的细胞毒活性。

GSK3β-IN-2 (Compound S01) 是一种强效的GSK3β抑制剂，IC50为0.35 nM。它能够激活Wnt β-catenin信号通路，从而促进神经发生和神经突的生长。此外，GSK3β-IN-2 可以降低由Aβ诱导的tau蛋白在Ser396位点的磷酸化水平，减少神经原纤维缠结的形成，并在斑马鱼模型中改善阿尔茨海默病。

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).

Wnt β-catenin agonist 2激活 Wnt β-catenin 信号传导，是一种有效的 Wnt 激动剂。 Wnt β-catenin agonist 2可用于与信号转导相关的疾病研究，与癌症侵袭转移密切相关。

Kirenol (Kirel) 是分离自 Siegesbeckia orientalis 中的，具有抗氧化、抗炎、抗过敏、抗关节炎活性，可用于缓解疼痛的研究。

Isoquercetin (3-Glucosylquercetin) 是天然存在的多酚，具有抗氧化，抗增殖和抗炎特性。它通过调节核因子-κB 转录调节系统调节一氧化氮合酶 2 的表达。它通过 Nrf2 ARE 抗氧化剂信号传导途径减轻乙醇诱导的肝毒性，氧化应激和炎症反应。它具有高生物利用度和低毒性，是预防糖尿病妊娠出生缺陷的有希望的候选药物。

Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation of the cAMP pathway. Via generating a transcriptionally active complex with β-catenin, CREB acts as a mediator of Wnt signaling.ICG-001 is an inhibitor of β-catenin CREB mediated transcription. The direct cellular target of ICG-001 is CREB. the inhibitory IC50of ICG-001 against β-catenin CREB mediated transcription was 3 μM. ICG-001 treatment at the concentration of 25 μM for 24h significantly increased caspase activity in both colon cancer cell lines SW480 and HCT116 cell lines but not in normal colonic epithelial cells CCD-841Co. In a cell growth inhibition assay, the IC50s of ICG-001 against SW480 and HCT116 cells were 4.43 μM and 5.95 μM, respectively.In a SW620 nude mouse xenograft model, an water-soluble analog of ICG-001 given at the dose of 150 mg kg i.v. once in every 2 days dramatically suppressed tumor growth. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg kg per day reversed pulmonary fibrosis. In a rat myocardial infarction model, ICG-001 was administrated subcutaneously at the dose of 50 mg kg day for 10 days which significantly improved cardiac contractile function after myocardial infarction in the rats.

Carboxylesterase-IN-2 是一种有效的 Carboxylesterase Notum 抑制剂（IC50 ≤10 nM）。Carboxylesterase-IN-2具有研究癌症疾病的潜力。

β-catenin-IN-6是一种针对Wnt β-catenin(典型的wingless相关整合位点)通路的抑制剂，能够抑制人类结直肠癌细胞的增殖，并在β-catenin RK3E小鼠模型上展现出效果。

BMP agonist 1 (compound 2 b) 是一种作用于骨形态发生蛋白 (BMP) 的小分子激动剂。该化合物能在C2C12细胞中与BMP协同作用，诱导其分化，其机制高度依赖BMP的活性信号传递路径。此外，BMP agonist 1 通过抑制GSK3β和增强β-catenin信号的表达，进而共同调控了Id2和Id3基因的表达。这种化合物主要用于研究骨骼相关疾病及损伤。

BIBO3304 (diTFA) 是口服有效、选择性的神经肽Y(NPY)Y1受体高效拮抗剂。对人类及大鼠Y1受体具高亲和力，IC50值分别为0.38和0.72 nM。BIBO3304 (diTFA) 通过Wnt/β-catenin信号通路促进骨肌腱愈合。

2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant