SKL2001

Catalog No.S8320 Batch:S832002

Technical Data

Formula	C₁₄H₁₄N₄O₃
Molecular Weight	286.29	CAS No.	909089-13-0
Solubility (25°C)*	In vitro	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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

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

Targets

Wnt/β-catenin ^[1]
(Cell-free assay)

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].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines HEK293 reporter and control cell lines Concentrations 20 μM Incubation Time 15 h Method 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.

Cell Assay:^{^[1]}

Cell lines
HEK293 reporter and control cell lines
Concentrations
20 μM
Incubation Time
15 h
Method
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.

References

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

Customer Product Validation

: 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]

: Data from [Data independently produced by , , Biochem Biophys Res Commun, 2017(484):586e591]

Selleck's SKL2001 has been cited by 48 publications

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
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
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
Critical role for ribonucleoside-diphosphate reductase subunit M2 in ALV-J-induced activation of Wnt/β-catenin signaling via interaction with P27 [ J Virol, 2023, 97(8):e0026723]	PubMed: 37582207
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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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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