SKL2001

製品コードS8320 バッチS832001

印刷

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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. 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^[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. 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^[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

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：

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
S100A6 Regulates nucleus pulposus cell apoptosis via Wnt/β-catenin signaling pathway: an in vitro and in vivo study [ Mol Med, 2024, 30(1):87]	PubMed: 38877413
High expression of LncRNA HOTAIR is a risk factor for temozolomide resistance in glioblastoma via activation of the miR-214/β-catenin/MGMT pathway [ Sci Rep, 2024, 14(1):26224]	PubMed: 39482401
PCSK9 inhibitor alleviates experimental pulmonary fibrosis-induced pulmonary hypertension via attenuating epithelial-mesenchymal transition by suppressing Wnt/β-catenin signaling in vivo and in vitro [ Front Med (Lausanne), 2024, 11:1509168]	PubMed: 39722825
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

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。