SKL2001

Catalog No.S8320 Batch:S832001

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 50 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
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