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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T63212	β-catenin-IN-3
	β-catenin-IN-3 是选择性的、有效的β- 连环蛋白 (β-catenin) 抑制剂(KD: 54.96 nM)，能够靶向 β-catenin 的一个隐变构调控位点，明显降低 β-catenin 驱动的癌细胞的活力。
T60485	DIF-3
	DIF-3 is a chemical compound that acts by activating GSK-3β to facilitate the degradation of cyclin D1 and c-Myc, resulting in reduced expression levels of these proteins. In addition, DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. This compound exerts a potent antiproliferative effect on the HeLa human cervical cancer cell line by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression [1].
T2310L	CHIR-99021 HCl CT99021 HCl,Laduviglusib HCl	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	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]。
T9138	Indirubin-3′-oxime Indirubin-3'-monoxime	GSK-3; CDK; JNK	Cell Cycle/Checkpoint; MAPK; PI3K/Akt/mTOR signaling; Stem Cells
	Indirubin-3′-oxime 是一种有效的细胞周期蛋白依赖性蛋白激酶抑制剂，是 indirubin 的合成衍生物。它可通过激活软骨细胞中的 Wnt/β-catenin 信号来促进身高增长，可能在阿尔茨海默病的神经元凋亡中发挥作用。
T62681	PDE5-IN-3
	PDE5-IN-3 (compound 11j) 是一种 PDE5 的有效抑制剂 (IC50: 1.57 nM)。PDE5-IN-3 对 EGFR 具有中度抑制作用 (IC50: 5.827 μM)。PDE5-IN-3 明显抑制 Wnt/β-catenin 通路，其 IC50 值为 1286.96 ng/mL。PDE5-IN-3 在 HepG2 细胞中诱导内在的凋亡线粒体途径。PDE5-IN-3 表现出显著的抗肿瘤效果。
T35551	Gallocyanine
	Gallocyanine is a small molecule blue dye used to stain nuclei. It is known to inhibit Dickkopf-1 (Dkk1), an antagonist of the Wnt pathway. Gallocyanine can disrupt the interaction of Dkk1 with its receptor LRP5/6 (IC50 = 3 μM), thereby activating Wnt/β-catenin signaling. Modulation of the Dkk1-LRP5/6 interaction via gallocyanine has been shown to inhibit prostaglandin J2-induced tau phosphorylation at serine396 in primary cortical neurons in vitro.
T75941	Foxy-5 TFA
	Foxy-5 TFA 是WNT5A 激动剂，是 WNT5A 的一个模拟肽，是Wnt 家族的非经典成员。Foxy-5 TFA 可在不影响β-catenin 激活的情况下触发胞浆游离钙信号传导，并可抑制上皮癌细胞的迁移和侵袭。Foxy-5 TFA 在原位小鼠模型中能有效降低 WNT5A 低表达的前列腺癌细胞的转移扩散。
T65994	(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide
	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...
T36684	Ipivivint
	Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5/6 phosphorylation[1].Ip...

化合物

Synonym: CT99021 HCl,Laduviglusib HCl

Target: GSK-3

Indirubin-3′-oxime

Cat.No: T9138

Synonym: Indirubin-3'-monoxime

Target: GSK-3, CDK, JNK

(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide

Cat. No.	Product Name	Target	Signaling Pathways
TL0007	Bisdemethoxycurcumin 双去甲氧基姜黄素,Curcumin III,Didemethoxycurcumin	Epigenetic Reader Domain; Wnt/beta-catenin	Chromatin/Epigenetic; Cytoskeletal Signaling; Stem Cells
	Bisdemethoxycurcumin (Curcumin III) 是一种具有抗炎及抗氧化作用的姜黄素。
T5S0754	Isoquercetin 3-Glucosylquercetin,Hirsutrin,Isoquercitrin,异槲皮苷,Quercetin 3-o-glucopyranoside,槲皮素-3-葡萄糖苷	NF-κB; Wnt/beta-catenin; NO Synthase	Cytoskeletal Signaling; Immunology/Inflammation; NF-κB; Stem Cells
	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。
T4S1943	Kirenol 奇壬醇,奇任醇,Kirel	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	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。