SKL2001

SKL2001 is a novel agonist of Wnt/β-catenin signaling pathway. SKL2001 suppresses colon cancer spheroid growth through regulation of the E-cadherin/β-Catenin complex. SKL2001 inhibited proliferation of colon cancer cells cultured in 3D spheroid and induced them accumulation in the G0/G1 phase of the cell cycle with a reduced c-myc level.

Product information

CAS Number: 909089-13-0

Molecular Weight: 286.29

Formula: C14H14N4O3

Synonym:

Wnt Agonist II

Chemical Name: 5-(Furan-2-yl)-N-(3-imidazol-1-ylpropyl)-1,2-oxazole-3-carboxamide

Smiles: O=C(NCCCN1C=NC=C1)C1C=C(ON=1)C1=CC=CO1

InChiKey: PQXINDBPUDNMPE-UHFFFAOYSA-N

InChi: InChI=1S/C14H14N4O3/c19-14(16-4-2-6-18-7-5-15-10-18)11-9-13(21-17-11)12-3-1-8-20-12/h1,3,5,7-10H,2,4,6H2,(H,16,19)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

SKL2001 is an agonist of the Wnt/β-catenin pathway, and also upregulates the expression of Axin2, a downstream target of the Wnt/β-catenin pathway, but shows no effect on NF-κB, p53 reporter activity and GSK-3β activity. SKL2001 causes osteoblast differentiation (20 and 40 μM) and suppresses preadipocyte differentiation (5, 10, and 30 μM) via the activation of the Wnt/β-catenin pathway. SKL2001 (5, 10, and 30 μM) stabilizes intracellular β-catenin in 3T3-L1 cells. SKL2001 (40 μM) significantly inhibits the proliferation of HCT116 spheroids independently of cytotoxicity and the inhibition is reversible; SKL2001 cuases cell cycle arrest in HCT116 spheroids. SKL2001 (40 μM) enhances round-shape spheroid formation and E-cadherin expression.

References:

1. Jie Z, Shen S, Zhao X, Xu W, Zhang X, Huang B, Tang P, Qin A, Fan S, Xie Z. Activating β-catenin/Pax6 axis negatively regulates osteoclastogenesis by selectively inhibiting phosphorylation of p38/MAPK. FASEB J. 2018 Dec 7:fj201801977R. doi: 10.1096/fj.201801977R. [Epub ahead of print] PubMed PMID: 30526042.
2. Huang HL, Tang GD, Liang ZH, Qin MB, Wang XM, Chang RJ, Qin HP. Role of Wnt/β-catenin pathway agonist SKL2001 in Caerulein-induced acute pancreatitis. Can J Physiol Pharmacol. 2018 Oct 16:1-8. doi: 10.1139/cjpp-2018-0226. [Epub ahead of print] PubMed PMID: 30326193.
3. Ohashi W, Yamamine N, Imura J, Hattori Y. SKL2001 suppresses colon cancer spheroid growth through regulation of the E-cadherin/β-Catenin complex. Biochem Biophys Res Commun. 2017 Nov 25;493(3):1342-1348. doi: 10.1016/j.bbrc.2017.09.161. Epub 2017 Sep 29. PubMed PMID: 28970068.

Products are for research use only. Not for human use.