SKL2001

製品コードS8320 バッチS832001

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₄H₁₄N₄O₃
	分子量	286.29	CAS No.	909089-13-0
Solubility (25°C)*	体外	DMSO	57 mg/mL (199.09 mM)
		Ethanol	57 mg/mL (199.09 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	SKL2001は、Wnt/β-カテニン経路の新規アゴニストです。これはAxin/β-カテニン相互作用を阻害します。
in vitro	SKL2001 upregulated β-catenin responsive transcription by increasing the intracellular β-catenin protein level and inhibited the phosphorylation of β-catenin at residues Ser33/37/Thr41 and Ser45, which would mark it for proteasomal degradation, without affecting CK1 and GSK-3β enzyme activities. This compound disrupted the Axin/β-catenin interaction, which is a critical step for CK1- and GSK-3β-mediated phosphorylation of β-catenin at Ser33/37/Thr41 and Ser45. The treatment of mesenchymal stem cells with this chemical promoted osteoblastogenesis and suppressed adipocyte differentiation, both of which were accompanied by the activation of Wnt/β-catenin pathway. It did not affect either NF-κB or p53 reporter activity and inhibits β-catenin phosphorylation without affecting GSK-3β activity.

製品説明

SKL2001は、Wnt/β-カテニン経路の新規アゴニストです。これはAxin/β-カテニン相互作用を阻害します。

in vitro

SKL2001 upregulated β-catenin responsive transcription by increasing the intracellular β-catenin protein level and inhibited the phosphorylation of β-catenin at residues Ser33/37/Thr41 and Ser45, which would mark it for proteasomal degradation, without affecting CK1 and GSK-3β enzyme activities. This compound disrupted the Axin/β-catenin interaction, which is a critical step for CK1- and GSK-3β-mediated phosphorylation of β-catenin at Ser33/37/Thr41 and Ser45. The treatment of mesenchymal stem cells with this chemical promoted osteoblastogenesis and suppressed adipocyte differentiation, both of which were accompanied by the activation of Wnt/β-catenin pathway. It did not affect either NF-κB or p53 reporter activity and inhibits β-catenin phosphorylation without affecting GSK-3β activity.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HEK293 reporter and control cell lines
	濃度	20 μM
	反応時間	15 h
	実験の流れ	The HEK293 reporter and control cell lines were established. The HEK293 reporter cells were inoculated into 384-well plates at 10 000 cells per well and grown for 24 h. Next, each compound in the chemical library (∼270 000) was added to at a final concentration of 20 μM. After 15 h, the plates were assayed for firefly luciferase activity.

参考

https://pubmed.ncbi.nlm.nih.gov/21826110/

カスタマーフィードバック

: Data from [Data independently produced by , , Lab Invest, 2018, 98(12):1527-1537]

: Data from [Data independently produced by , , Life Sci, 2018, 197:91-100]

: Data from [Data independently produced by , , Biochem Biophys Res Commun, 2017, 486(1):49-56]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Circ-CCT2 Activates Wnt/β-catenin Signaling to Facilitate Hepatoblastoma Development by Stabilizing PTBP1 mRNA [ Cellular and Molecular Gastroenterology and Hepatology, October 20 2023, 175-197]	PubMed: 37866478
LINC00115 promotes stemness and inhibits apoptosis of ovarian cancer stem cells by upregulating SOX9 and inhibiting the Wnt/β-catenin pathway through competitively binding to microRNA-30a [ Cancer Cell International, July 08 2021, 360]	PubMed: 34238293
Role of Wnt/β-catenin pathway agonist SKL2001 in Caerulein-induced acute pancreatitis [ Canadian Journal of Physiology and Pharmacology, January 2019, 15-22]	PubMed: 30326193
Methazolamide Attenuates the Development of Diabetic Cardiomyopathy by Promoting β-Catenin Degradation in Type 1 Diabetic Mice [ Diabetes, April 01 2022, 795-811]	PubMed: 35043173
CD36 enrichment in HER2-positive mesenchymal stem cells drives therapy refractoriness in breast cancer [ J Exp Clin Cancer Res, 2025, 44(1):19]	PubMed: 39833955
Centromere protein I facilitates breast cancer tumorigenesis and disease progression through modulation of Wnt/β-Catenin signaling [ Cancer Cell Int, 2025, 25(1):348]	PubMed: 41074145
Lung endothelium exploits susceptible tumor cell states to instruct metastatic latency [ Nat Cancer, 2024, 10.1038/s43018-023-00716-7]	PubMed: 38308117
MEN1 Deficiency-Driven Activation of the β-Catenin-MGMT Axis Promotes Pancreatic Neuroendocrine Tumor Growth and Confers Temozolomide Resistance [ Adv Sci (Weinh), 2024, 11(35):e2308417]	PubMed: 39041891
Tumor-derived Exosomal ENO2 Modulates Polarization of Tumor-associated Macrophages through Reprogramming Glycolysis to Promote Progression of Diffuse Large B-cell Lymphoma [ Int J Biol Sci, 2024, 20(3):848-863]	PubMed: 38250157
β-catenin inhibition disrupts the homeostasis of osteogenic/adipogenic differentiation leading to the development of glucocorticoid-induced osteonecrosis of the femoral head [ Elife, 2024, 12RP92469]	PubMed: 38376133

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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