SKL2001
(Synonyms: Wnt Agonist II) 目录号 : GC16382
SKL2001是一种Wnt/β-catenin通路激动剂。SKL2001通过破坏Axin/β-catenin的相互作用稳定细胞内的β-catenin，可用于调控间充质干细胞分化。
Cas No.:909089-13-0
Sample solution is provided at 25 µL, 10mM.
SKL2001 is an agonist of the Wnt/β-catenin pathway. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction, and can be applied to regulate mesenchymal stem cell differentiation[1].
SKL2001 (5, 10, and 30μM; 3d) consistently induced the accumulation of intracellular β-catenin and inhibited the expression of C/EBPα and PPARγ. The exposure of 3T3-L1 and ST2 cells to SKL2001 resulted in a concentration-dependent decrease in lipid droplet accumulation in response to insulin[1]. SKL2001 (10, 30μM; 15h) 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[1].Treatment of ECs with SKL2001 at 30μM for 12h induced the expressions of MALAT1, ZO-1 and Occludin[2].
SKL2001 (6mg/kg; ip; 7d) treatment results in a decrease in the permeability of the aortic wall of the mice[2].In the doxorubicin mouse model, SKL2001 (4mg/kg; ip; 7d) stimulated rCFs to activate the Wnt/β-catenin pathway, inducing cardiac dysfunction and myocardial fibrosis in mice[3].
References:
[1]. Gwak J, Hwang S G, Park H S, et al. Small molecule-based disruption of the Axin/β-catenin protein complex regulates mesenchymal stem cell differentiation[J]. Cell research, 2012, 22(1): 237-247.
[2]. Yang F, Zhang Y, Zhu J, et al. Laminar flow protects vascular endothelial tight junctions and barrier function via maintaining the expression of long non-coding RNA MALAT1[J]. Frontiers in Bioengineering and Biotechnology, 2020, 8: 647.
[3]. Yuan M, Shi H, Wang B, et al. Targeting SOCS2 alleviates myocardial fibrosis by reducing nuclear translocation of β-catenin[J]. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research, 2024, 1871(7): 119804.
SKL2001是一种Wnt/β-catenin通路激动剂。SKL2001通过破坏Axin/β-catenin的相互作用稳定细胞内的β-catenin，可用于调控间充质干细胞分化[1]。
SKL2001（5、10、30μM；3d）能持续诱导细胞内β-catenin的积累，抑制C/EBPα和PPARγ的表达。将 3T3-L1 和 ST2 细胞暴露于SKL2001会导致对胰岛素反应的脂滴积聚的浓度依赖性减少[1]。SKL2001（10、30μM；15h）通过增加细胞内β-catenin蛋白水平上调β-catenin反应性转录，抑制β-catenin在Ser33/37/Thr41和Ser45残基的磷酸化[1]。用30μM的SKL2001处理EC细胞12h，可诱导MALAT1、ZO-1和Occludin的表达[2]。
SKL2001（6mg/kg；ip；7d）可降低小鼠主动脉壁的通透性[2]。在多柔比星小鼠模型中，SKL2001（4mg/kg；ip；7d）刺激rCFs激活Wnt/β-catenin通路，诱导小鼠心功能障碍和心肌纤维化[3]。
| Cell experiment [1]: | |
|
Cell lines |
3T3-L1 and ST2 cells |
|
Preparation Method |
SKL2001 (5, 10, and 30μM) was administered to cells during adipocyte differentiation for 3 days. The total proteins were prepared and subjected to western blotting with anti-β-catenin, anti-PPARγ and anti-C/EBPα antibodies. |
|
Reaction Conditions |
5, 10, and 30μM; 3d |
|
Applications |
SKL2001 consistently induced the accumulation of intracellular β-catenin and inhibited the expression of C/EBPα and PPARγ. The exposure of 3T3-L1 and ST2 cells to SKL2001 resulted in a concentration-dependent decrease in lipid droplet accumulation. |
| Animal experiment [2]: | |
|
Animal models |
Arterial Endothelial Barrier Model |
|
Preparation Method |
Mice were injected intraperitoneally with SKL2001 (6mg/kg in 100μL of DMSO), XAV939 (4mg/kg in 100μL of DMSO) or DMSO (100μL) daily for 7 days. The arterial endothelial permeability to Evans blue dye was assessed. |
|
Dosage form |
6mg/kg; ip; 7d |
|
Applications |
Aortic wall permeability to Evans blue was reduced in SKL2001-treated mice. |
|
References: |
|
| Cas No. | 909089-13-0 | SDF | |
| 别名 | Wnt Agonist II | ||
| 化学名 | N-(3-(1H-imidazol-1-yl)propyl)-5-(furan-2-yl)isoxazole-3-carboxamide | ||
| Canonical SMILES | O=C(C1=NOC(C2=CC=CO2)=C1)NCCCN3C=CN=C3 | ||
| 分子式 | C14H14N4O3 | 分子量 | 286.29 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 25 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.493 mL | 17.4648 mL | 34.9296 mL |
| 5 mM | 0.6986 mL | 3.493 mL | 6.9859 mL |
| 10 mM | 0.3493 mL | 1.7465 mL | 3.493 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet