SKL2001

製品コードS8320 バッチS832002

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 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction.
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. SKL2001 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 SKL2001 promoted osteoblastogenesis and suppressed adipocyte differentiation, both of which were accompanied by the activation of Wnt/β-catenin pathway. SKL2001 did not affect either NF-κB or p53 reporter activity and inhibits β-catenin phosphorylation without affecting GSK-3β activity^[1].

製品説明

SKL2001 is a novel agonist of the Wnt/β-catenin pathway. It disrupts the Axin/β-catenin interaction.

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. SKL2001 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 SKL2001 promoted osteoblastogenesis and suppressed adipocyte differentiation, both of which were accompanied by the activation of Wnt/β-catenin pathway. SKL2001 did not affect either NF-κB or p53 reporter activity and inhibits β-catenin phosphorylation without affecting GSK-3β activity^[1].

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

[1] Gwak J, et al. Cell Res. 2012, 22(1):237-47.

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：

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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
Long non-coding RNA NRSN2-AS1 promotes ovarian cancer progression through targeting PTK2/β-catenin pathway [ Cell Death Dis, 2023, 14(10):696]	PubMed: 37875515
Circ-CCT2 Activates Wnt/β-catenin Signaling to Facilitate Hepatoblastoma Development by Stabilizing PTBP1 mRNA [ Cell Mol Gastroenterol Hepatol, 2023, 10.1016/j.jcmgh.2023.10.004]	PubMed: 37866478
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Adipocyte-derived CCDC3 promotes tumorigenesis in epithelial ovarian cancer through the Wnt/ß-catenin signalling pathway [ Biochem Biophys Rep, 2023, 35:101507]	PubMed: 37601453
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PROX1 promotes breast cancer invasion and metastasis through WNT/β-catenin pathway via interacting with hnRNPK [ Int J Biol Sci, 2022, 18(5):2032-2046]	PubMed: 35342346
A specific upregulated lncRNA in colorectal cancer promotes cancer progression [ JCI Insight, 2022, e158855]	PubMed: 35617032

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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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